와파린
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와파린 속성
- 녹는점
- 162-164 °C(lit.)
- 끓는 점
- 356°C
- 밀도
- 1.1411 (rough estimate)
- 증기압
- 0.09 at 22 °C (NIOSH, 1997)
- 굴절률
- 1.4434 (estimate)
- 인화점
- 2℃
- 저장 조건
- 2-8°C
- 용해도
- Soluble in benzene, 1,4-dioxane (Weast, 1986), and acetone (Sax and Lewis, 1987). Moderately soluble in methanol, ethanol, isopropanol, and some oils (Windholz et al., 1983). Also soluble in toluene.
- 물리적 상태
- 수정 같은
- 산도 계수 (pKa)
- pKa 4.90±0.01(H2O t = 25±0.5 I = 0.15 (KCl))(Approximate)
- 색상
- 무색의
- 냄새
- 냄새 없는
- 수용성
- 실질적으로 불용성
- Merck
- 13,10097
- BRN
- 8868198
- 노출 한도
- NIOSH REL: TWA 0.1 mg/m3, IDLH 100 mg/m3; OSHA PEL: 0.1 mg/m3; ACGIH TLV: TWA 0.1 mg/m3.
- LogP
- 2.600
- CAS 데이터베이스
- 81-81-2(CAS DataBase Reference)
안전
- 위험 및 안전 성명
- 위험 및 사전주의 사항 (GHS)
위험품 표기 | T,T+,Xn,F | ||
---|---|---|---|
위험 카페고리 넘버 | 61-48/25-52/53-28-21-36-20/21/22-11 | ||
안전지침서 | 53-45-61-52-36/37-28-26-16 | ||
유엔번호(UN No.) | UN 2811 6.1/PG 1 | ||
WGK 독일 | 3 | ||
RTECS 번호 | GN4550000 | ||
위험 등급 | 6.1(a) | ||
포장분류 | I | ||
HS 번호 | 29322090 | ||
유해 물질 데이터 | 81-81-2(Hazardous Substances Data) | ||
독성 | EC50 (24-hour) for Daphnia magna 88.8 mg/L (Lilius et al., 1995); acute oral LD50 for rats 186 mg/kg (Hartley and Kidd, 1987), 3 mg/kg (RTECS, 1985) | ||
IDLA | 100 mg/m3 | ||
기존화학 물질 | KE-20784 | ||
유해화학물질 필터링 | 97-1-219 | ||
중점관리물질 필터링 | 별표2-19 | ||
암, 돌연변이성물질 필터링 | 39 | ||
함량 및 규제정보 | 물질구분: 유독물질; 혼합물(제품)함량정보: 왈파린과 그 염류 및 그 중 하나를 0.1% 이상 함유한 혼합물 |
와파린 C화학적 특성, 용도, 생산
개요
Warfarin was the first of the synthetic anticoagulant rodenticides with structural features inspired by a natural product (88). This prototype coumarin derivative was developed in the 1940s by systematically altering the structure of dicumarol (46), recognized earlier as the causative agent of the sweet clover disease causing severe bleeding in grazing cattle (89). These rodenticides act by inhibiting the oxidoreductive recycling of vitamin K, a cofactor necessary for prothrombin synthesis involved in blood coagulation.화학적 성질
Warfarin is a colorless, odorless crystalline solid.용도
Coumadin is widely used as an anticoagulant for various systemic diseases such as venous thromboembolism, cardiac arrhythmia, following myocardial infarction, and hematologic abnormalities, among others. However, the efficacy of coumadin for CRVO is not established. It was reported that 13 of 354 patients taking warfarin developed CRVO despite maintaining therapeutic levels of the anticoagulant.주요 응용
Warfarin is an anti-coagulant used to prevent heart attacks, strokes, and the formation of blood clots. It interferes with the use of vitamin K in the required carboxylation of several vitamin K-dependent proteins in the clotting cascade, preventing the initiating of clotting. (±)-Warfarin is a racemic mixture of 2 optically active isomers. (±)-Warfarin has a half-life of 36-42 hours in circulation, bound to plasma proteins, and accumulates in the liver, where the two isomers are metabolized by different pathways.World Health Organization (WHO)
Warfarin, a coumarin anticoagulant, was introduced into medicine in 1950 for the prevention and managementof thrombo-embolic disorders. Its use during the first trimester of pregnancy has been associated with birth malformations, particularly in relation to cranial and limb development, and there have been reports of foetal death due to haemorrhage following administration of the drug during the late stages of pregnancy. The decision of the Egyptian agency to requrie a warning regarding teratogenicity to be included in the approved information of products containing warfarin beings the text of the package insert in line with those approved in other countries. Warfarin is included in the WHO Model List of Essential Drugs.반응 프로필
Warfarin is incompatible with the following: Strong oxidizers .건강위험
Warfarin is classified as very toxic. Probable oral lethal dose in humans is 50-500 mg/kg, between 1 teaspoon and 1 ounce for a 150 lb. person. Material is an anticoagulant. Toxic effects other than hemorrhage are rarely seen in humans. Material is believed to be teratogenic in humans. Persons with a history of blood disorders with bleeding tendencies would be expected to be at increased risk from exposure.화재위험
Contact with strong oxidizers may cause fires and explosions. Toxic gases and vapors (e.g., carbon monoxide) may be released in heating to decomposition. Avoid strong oxidizers.농업용
Rodenticide: Warfarin and its sodium salt is an anticoagulant rodenticide used for controlling rats and house mice in and around homes, animal and agricultural premises, and commercialand industrial sites. It is effective in very low dosages. About a week is required before a marked reduction in the rodent population is noticeable. Rodents do not become bait-shy after once tasting warfarin; they continue to consume it until its anti-clotting properties have produced death through internal hemorrhaging. It can be used year-after-year wherever a rodent problem exists. Warfarin and its sodium salt are only slightly dangerous to humans and domestic animals when used as directed, but care must be taken with young pigs, which are especially susceptible. The sodium salt is also used to treat people with blood hypercoagulation problems. Registered for use in EU countries . Registered for use in the U.S.Pharmaceutical Applications
A group of naturally occurring antibiotics chemically related to the coumarin group of anticoagulants. The best known is novobiocin, but a few naturally occurring coumarins and some semisynthetic derivatives have been studied. They share a narrow range of antimicrobial activity largely directed against aerobic Gram-positive organisms. Novobiocin inhibits susceptible strains of Staph. aureus (including β-lactamaseproducing and methicillin-resistant strains), Str. pyogenes and Str. pneumonia at a concentration of 0.1–2 mg/L and it has been considered for the treatment of infection with multiresistant Staph. aureus and other Gram-positive cocci. However, since resistance arises readily and side effects are common, the general consensus is that it no longer has a place in antibacterial therapy.There has been some revived interest in coumarins as potentiating agents of antineoplastic drugs.
상품명
ARAB RAT DETH®; ATROMBINE-K®; BRUMIN®; COMPOUND 42®; D-CON®; CO- RAX®; DETHMORE®; EAGLES-7®; EASTERN STATES DUOCIDE®; GROVEX SEWER BAIT®; HOPKINS BAR BAIR®; HOPKINS COV-R-TOX®; HOPKINS RODEX®; KILLGERM SEWARIN P®; KILMOL®; LIQUA-TOX®; MAR-FIN®; MOUSE PAK®; PLUSBAIT®; RAT-A-WAY®; RAT-B-GON®; RAT-O-CIDE®; RAT-GARD®; RAT & MICE BAIT®; RATRON®; RATS-NO-MORE®; RATTUNAL®; RAX®; RCR SQUIRREL KILLER®; RENTOKIL®; RENTOKIL BIOTROL®; RODEX BLOX®; RODENTEX®; RO- DETH®; RODEX®; ROUGH & READY MOUSE MIX®; SAKARAT®; SOLFARIN®; SOREXA PLUS®; SOREX CR1®; SEWARIN®; SPRAY-TROL BRANCH®; TWIN LIGHT RAT AWAY®; RODEN-TROL®; WARFARAT®; WARF COMPOUND®; VAMPIRINIP® Sodium Salt: ATHROMBIN®; LIQUA-TOX®; PANWARFIN®; RATSUL SOLUBLE®; TINTORANE®; VARFINE®; WARAN®; WARCOUMIN®; WARFILONE®Mechanism of action
Warfarin sodium is rapidly and completely absorbed (~100% bioavailability) following oral, intramuscular, intravenous, or rectal administration. Peak plasma concentrations occur at approximately 3 hours. Its anticoagulant effect is not immediately present, however, following initiation of therapy. Instead, a delay in onset of anticoagulation occurs while the clotting factors with normal activity are cleared and those that have not been carboxylated because of the actions of warfarin reach physiologically significant levels. On average, this delay is approximately 5 hours for factor V turnover and 2 to 3 days for factor II (thrombin). Consequently, because of the rapid decline in protein C levels, the anticoagulated state frequently is preceded by a period of hypercoagulability (25).Warfarin also is highly protein bound (95–99%) and, as a result, has numerous interactions with other drugs. The free drug (i.e., that not bound to plasma proteins) is the active constituent. Therefore, any other substance that displaces bound drug from protein binding sites increases the levels of free drug and, as a result, can cause warfarin toxicity, which usually is manifested by hemorrhage. The volume of distribution(Vd) is quite small (0.1–0.2 L/kg), and the plasma half-life is quite long, both of which presumably result from the high degree of plasma protein binding.
Pharmacokinetics
Warfarin sodium is rapidly and completely absorbed (~100% bioavailability) following oral, intramuscular, intravenous, or rectal administration. Peak plasma concentrations occur at approximately 3 hours. Its anticoagulant effect is not immediately present, however, following initiation of therapy. Instead, a delay in onset of anticoagulation occurs while the clotting factors with normal activity are cleared and those that have not been carboxylated because of the actions of warfarin reach physiologically significant levels. On average, this delay is approximately 5 hours for factor V turnover and 2 to 3 days for factor II (thrombin). Consequently, because of the rapid decline in protein C levels, the anticoagulated state frequently is preceded by a period of hypercoagulability (25).Warfarin also is highly protein bound (95–99%) and, as a result, has numerous interactions with other drugs. The free drug (i.e., that not bound to plasma proteins) is the active constituent. Therefore, any other substance that displaces bound drug from protein binding sites increases the levels of free drug and, as a result, can cause warfarin toxicity, which usually is manifested by hemorrhage. The volume of distribution(Vd) is quite small (0.1–0.2 L/kg), and the plasma half-life is quite long, both of which presumably result from the high degree of plasma protein binding.
Safety Profile
A human poison by ingestion. Poison by inhalation and intravenous routes. Moderately toxic by skin contact, subcutaneous, and intraperitoneal routes. Human systemic effects by ingestion: hemorrhage, ulceration or bleeding from small intestine, blood clotting factor change. Human reproductive effects by ingestion and intramuscular routes: fetal death and physical abnormalities at birth. Human teratogenic effects include developmental abnormalities of the craniofacial area, musculoskeletal system, and respiratory system. An experimental teratogen. Other experimental reproductive effects. Used as an oral anticoagulant and as a rodenticide. When heated to decomposition it emits acrid smoke and fumes.잠재적 노출
Warfarin is used as an oral anticoagulant and as a rodenticide or rat poison.Carcinogenicity
No data suggest that warfarin is either mutagenic or carcinogenic.환경귀착
Photolytic. Warfarin may undergo direct photolysis since the pesticide showed an absorption maximum of 330 nm (Gore et al., 1971)Chemical/Physical. The hydrolysis half-lives at 68.0°C and pH values of 3.09, 7.11 and 10.18 were calculated to be 12.9, 57.4 and 23.9 days, respectively. At 25°C and pH 7, the half-life was estimated to be 16 years (Ellington et al., 1986)
신진 대사
Warfarin and other coumarin derivatives undergo extensive hepatic oxidative metabolism catalyzed by CYP2C9 isozyme to give 6- and 7-hydroxywarfarins as the major inactive metabolites. Warfarin also undergoes, to a lesser extent, reductive metabolism of the ketone on the C-3 side chain to a pair of pharmacologically active, diastereomeric 2-hydroxywarfarins). Almost no unchanged drug is excreted in the urine. As expected, those individuals with compromised hepatic function are at greater risk for warfarin toxicity secondary to diminished clearance. Many of the drug–drug interactions are associated with enhanced or inhibited metabolism of warfarin via CYP2C9 induction or inhibition. Many additional drugs and conditions have profound effects on warfarin therapy. A partial list of these factors is shown in Table 31.2.운송 방법
UN3027 Coumarin derivative pesticides, solid, toxic, Hazard Class: 6.1; Labels: 6.1-Poisonous materials. UN2811 Toxic solids, organic, n.o.s., Hazard Class: 6.1; Labels: 6.1-Poisonous materials, Technical Name Required.Purification Methods
dl-Warfarin crystallises from EtOH or MeOH. UV: max at 308nm ( 13,610) in H2O. The acetate has m 117-118o, the O-triflate has m 90-91o, and the 2,4-dinitrophenylhydrazone has m 215-216o. It is an effective anticoagulant and rodenticide. [West et al. J Am Chem Soc 83 2676 1961, HPLC: Banfield & Rowland J Pharm Sci 72 921 1983, Beilstein 17 III/IV 6794.] dl-Warfarin is resolved via recrystallisation of the quinidine salt, and the free acids are recrystallised (70g) from 600mL of 80% aqueous Me2CO. Large prismatic crystals of the pure enantiomers are obtained by slow crystallisation from Me2CO or AcOH. The solubilities of the pure enantiomers at 25o are 11.2% in Me2CO and 2.6% in AcOH, whereas the racemate has solubilities of 6.5% in Me2CO and 2% in AcOH. The IR spectra are the same with max (CHCl3) at 2.78 (w), 5.88, 6.16 and 6.38. [West et al. J Am Chem Soc 83 2676 1961, Cbz-proline diastereoisomeric esters were used for HPLC analysis: Banfield & Rowland J Pharm Sci 72 921 1983.] Poisonous, anticoagulant and rodenticide.비 호환성
Incompatible with oxidizers (chlorates, nitrates, peroxides, permanganates, perchlorates, chlorine, bromine, fluorine, etc.); contact may cause fires or explosions. Keep away from alkaline materials, strong bases, strong acids, oxoacids, epoxides. Dust mixtures with air may cause explosion.폐기물 처리
Consult with environmental regulatory agencies for guidance on acceptable disposal practices. Generators of waste containing this contaminant (≥100 kg/mo) must conform to EPA regulations governing storage, transportation, treatment, and waste disposal. Incineration.와파린 준비 용품 및 원자재
원자재
Mother powder
4-히드록시쿠마린
살리실산
파라핀 왁스
톨루엔
나트륨
아스피린
Raw powder
옥수수씨가루
벤즈알데하이드
N-부틸렌
염화 티오닐
황산
수산화나트륨
4-페닐부트-3-엔-2-온
trans-4-Phenyl-3-buten-2-one
Warfarin Impurity E
DL-Valine
준비 용품
와파린 공급 업체
글로벌( 223)공급 업체
공급자 | 전화 | 이메일 | 국가 | 제품 수 | 이점 |
---|---|---|---|---|---|
Henan Tianfu Chemical Co.,Ltd. | +86-0371-55170693 +86-19937530512 |
info@tianfuchem.com | China | 21695 | 55 |
Hubei XinRunde Chemical Co., Ltd. | +8615102730682 |
bruce@xrdchem.cn | CHINA | 566 | 55 |
Hefei TNJ Chemical Industry Co.,Ltd. | +86-0551-65418679 +86-18949832763 |
info@tnjchem.com | China | 2989 | 55 |
Shanxi Naipu Import and Export Co.,Ltd | +86-13734021967 +8613734021967 |
kaia@neputrading.com | China | 1011 | 58 |
career henan chemical co | +86-0371-86658258 |
sales@coreychem.com | China | 29914 | 58 |
Hubei Jusheng Technology Co.,Ltd. | 18871490254 |
linda@hubeijusheng.com | CHINA | 28180 | 58 |
Hubei xin bonus chemical co. LTD | 86-13657291602 |
linda@hubeijusheng.com | CHINA | 22968 | 58 |
Chongqing Chemdad Co., Ltd | +86-023-61398051 +8613650506873 |
sales@chemdad.com | China | 39916 | 58 |
CONIER CHEM AND PHARMA LIMITED | +8618523575427 |
sales@conier.com | China | 47465 | 58 |
Hefei TNJ Chemical Industry Co.,Ltd. | 0551-65418671 |
sales@tnjchem.com | China | 34572 | 58 |
와파린 관련 검색:
쿠마린 4 코우마린 부틸레이티드 하이드록시 아니솔 4-히드록시쿠마린 7-하이드록시쿠마린 페닐히드라진 6-히드록시쿠마린 부틸산화 히드록시톨루엔 와파린 덱스트로와파린 와파린
PHENYL VALERATE
Tetrahydro-4H-pyran-4-one
Tetrahydropyran
CHLOROPHOSPHONAZO III
Centchroman
WARFARIN SODIUM USP 26,WARFARIN SODIUM BP USP,WARFARIN SODIUM CRYSTALLINE CLATHRATE,warfarin,sodiumderiv
DICUMAROL