Grapiprant

Grapiprant 구조식 이미지
카스 번호:
415903-37-6
상품명:
Grapiprant
동의어(영문):
N-((4-(2-ethyl-4,6-dimethyl-1H-imidazo[4,5-c]pyridin-1-yl)phenethyl)carbamoyl)-4-methylbenzenesulfonamide;RQ 7;MR 10A7;AAT 007;CS-1556;Grprant;CJ-023423;Grapiprant;RQ 00000007;CAS#415903-37-6
CBNumber:
CB03054518
분자식:
C26H29N5O3S
포뮬러 무게:
491.61
MOL 파일:
415903-37-6.mol
MSDS 파일:
SDS

Grapiprant 속성

녹는점
>151°C (dec.)
밀도
1.29±0.1 g/cm3(Predicted)
저장 조건
Sealed in dry,Store in freezer, under -20°C
용해도
DMSO에 용해됨(최대 10mg/ml)
산도 계수 (pKa)
5.19±0.10(Predicted)
물리적 상태
고체
물리적 상태
단단한 모양
색상
회백색
안정성
제공된 대로 구매일로부터 1년 동안 안정적입니다. DMSO 용액은 -20°C에서 최대 3개월 동안 보관할 수 있습니다.
InChIKey
HZVLFTCYCLXTGV-UHFFFAOYSA-N
SMILES
C1(S(NC(NCCC2=CC=C(N3C4C=C(C)N=C(C)C=4N=C3CC)C=C2)=O)(=O)=O)=CC=C(C)C=C1

안전

Grapiprant C화학적 특성, 용도, 생산

개요

Prostaglandin E2 (PGE2) activates four E prostanoid (EP) receptors, EP1-4. EP4 is a Gs protein-coupled receptor that, by elevating the second messenger cAMP, plays important roles in bone formation and resorption, cancer, and atherosclerosis. CJ-023423 is a potent and selective antagonist of the EP4 receptor (Ki = 13 and 20 nM for human and rat EP4, respectively). It inhibits PGE2-evoked elevation in intracellular cAMP in cells and, in vivo, reduces thermal hyperalgesia induced by intraplantar injection of PGE2. CJ-023423 reduces acute and chronic inflammatory pain in different mouse models.

용도

CJ-023423 is a potent and selective antagonist of E prostanoid 4 (EP4) receptor.

Biological Functions

Grapiprant (CJ-023423) is an orally available, a potent and selective EP4 receptor antagonist that exhibits significant inhibitory effects on paw swelling, inflammatory biomarkers, synovial inflammation and bone destruction in AIA rats. Grapiprant is highly selective for the human EP4 receptor over other human prostanoid receptor subtypes. It also inhibits PGE2-evoked elevation in intracellular cAMP at the human and rat EP4 receptors with pA2 of 8.3 and 8.2 nM, respectively. In vivo, oral administration of grapiprant significantly reduces thermal hyperalgesia induced by intraplantar injection of PGE2 (ED50 = 12.8 mg/kg). It is also effective in models of acute and chronic inflammatory pain. Grapiprant significantly reduces mechanical hyperalgesia in the carrageenan model. Furthermore, it significantly reverses complete Freund′s adjuvant-induced chronic inflammatory pain response. It produces antihyperalgesic effects in animal models of inflammatory pain. Grapiprant is approved and widely used for treatment of osteoarthritis related pain in dogs. Grapiprant is classify as a non-cyclooxygenase inhibiting non-steroidal anti-inflammatory drug (NSAID).

Grapiprant 준비 용품 및 원자재

원자재

준비 용품


Grapiprant 공급 업체

글로벌( 97)공급 업체
공급자 전화 이메일 국가 제품 수 이점
Hpets Biotech Company (Chongqing) Co.,ltd
+8613340353813
info@hanpets.com China 26 58
Hangzhou ICH Biofarm Co., Ltd
+undefined8613073685410
sales@ichemie.com China 985 58
ATK CHEMICAL COMPANY LIMITED
+undefined-21-51877795
ivan@atkchemical.com China 32480 60
BOC Sciences
+1-631-485-4226
inquiry@bocsci.com United States 19553 58
TopScience Biochemical
00852-68527855
info@itopbiochem.com China Hong Kong 902 58
ANHUI WITOP BIOTECH CO., LTD
+8615255079626
eric@witopchemical.com China 23556 58
Guangzhou TongYi biochemistry technology Co.,LTD
+8613073028829
mack@tongyon.com China 2996 58
InvivoChem
+1-708-310-1919 +1-13798911105
sales@invivochem.cn United States 6393 58
Nanjing Doge Biomedical Technology Co., Ltd
+86-25-58227606 +86-15305155328
sales@dogechemical.com China 4128 58
LEAP CHEM CO., LTD.
+86-852-30606658
market18@leapchem.com China 24738 58

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