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MK-0822

Bioactivity In vitro In vivo Features
MK-0822
MK-0822 structure
CAS No.
603139-19-1
Chemical Name:
MK-0822
Synonyms
MK-0822;ODANACATIB;Unii-N673F6W2vh;Odanacatib, >=98%;Odanacatib(Mk0822);(MK0822,Odanacatib);Odanacatib,MK-0822,MK0822;N-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl}-L-leucinamide;(S)-N-(1-cyanocyclopropyl)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide;(2S)-N-(1-cyanocyclopropyl)-4-fluoro-4-methyl-2-[[(1S)-2,2,2-trifluoro-1-[4-(4-methylsulfonylphenyl)phenyl]ethyl]amino]pentanamide
CBNumber:
CB52455399
Molecular Formula:
C25H27F4N3O3S
Formula Weight:
525.564
MOL File:
603139-19-1.mol

MK-0822 Properties

Density 
1.35

MK-0822 price More Price(4)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 21466 Odanacatib ≥98% 603139-19-1 1mg $45 2018-11-19 Buy
Cayman Chemical 21466 Odanacatib ≥98% 603139-19-1 5mg $191 2018-11-19 Buy
Cayman Chemical 21466 Odanacatib ≥98% 603139-19-1 10mg $360 2018-11-19 Buy
Cayman Chemical 21466 Odanacatib ≥98% 603139-19-1 25mg $788 2018-11-19 Buy

MK-0822 Chemical Properties,Uses,Production

Bioactivity

Odanacatib (MK-0822) is an effective and selective neutral inhibitor for cathepsin K(human /rabbit) and IC50 is 0.2 nM/1 nM.  It has high selectivity for off-target cathepsin B, L, S. Phase 3。

In vitro

In vitro, Odanacatib acts on cathepsin K with high inhibitory activity and selectivity with IC50 of 0.2 nM and 1 nM when it acts on cathepsin K of human and rabbits. Odanacatib is also effective in all human enzyme experiments with IC50 of 5 nM.

In vivo

With a dosage of 10 mg/kg acting on preclinical rats, Odanacatib has good pharmacokinetic characteristics such as scavenging activity(Cl: 2 mL kg-1 min-1), low distribution (Vdss: 1.1 L kg-1), half-life(T1/2: 6 h) and Orally bioavailable (F: 8%).In addition, Odanacatib has a good metabolic stability if it acts on the Parental rats with 96% recovery of live. With the dosage of 9 µM, Odanacatib can significantly Increase the Proximal femur bone mineral density (BMD) (7.8%), femoral neck BMD (10.8%) and thighs greater trochanter BMD (6.5%). Long-term treatment with Odanacatib on skeletal matured macaque which is lack of estrogen can efficiently inhibit the bone metabolism, and will not reduce the number of osteoclast. It can also maintain the biomechanics properties of nonhuman primates with Ovary resection (OVX).

Features

Odanacatibis an effective and selective neutral inhibitor for cathepsin K

Enzyme inhibitor

This investigational osteoporosis/bone-metastasis drug (FW = 525.56 g/mol; CAS 603139-19-1), also known by the code name MK-0822 and its systematic name N-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro- 1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl}-L-leucinamide, targets the cathepsin K, a unique collagenolytic lysosomal cysteine protease that is secreted, thereby facilitating bone resorption by cleaving type-1 collagen under acidic pH. Cathepsin K exhibits a unique cleavage pattern of type I collagen molecules that is fundamentally different from that of other endogenous collagenases. Women receiving ODN (10-50 mg) for 5 years had gains in spine and hip bone mineral density (BMD), showing larger reductions in bone resorption than bone formation markers. Significantly, discontinuation of ODN resulted in reversal of treatment effects. An odanacatib synthesis, which describes a novel stereospecific SN2 triflate displacement of a chiral a-trifluoromethylbenzyl triflate with (S)-g-fluoroleucine ethyl ester, achieves a 61% overall yield in 6 steps.

MK-0822 Preparation Products And Raw materials

Raw materials

Preparation Products


MK-0822 Suppliers

Global( 94)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Alpha Biopharmaceuticals Co., Ltd
0086-411-39042497
0086-411-39042693 sales@alphabiopharm.com China 920 58
Nanjing ChemLin Chemical Industry Co., Ltd.
025-83697070;product@chemlin.com.cn
product@chemlin.com.cn CHINA 3015 60
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 29979 58
Biochempartner
0086-13720134139
candy@biochempartner.com CHINA 969 58
Hubei xin bonus chemical co. LTD
86-13657291602
027-59338440 sales@guangaobio.com CHINA 23049 58
BOC Sciences
1-631-619-7922
1-631-614-7828 inquiry@bocsci.com United States 20115 58
Chongqing Chemdad Co., Ltd +86-13650506873
sales@chemdad.com CHINA 30864 58
WuYan Pharmaceutical Technology (Shanghai) Co., Ltd. 0512-53995837,13371908063
021-61114075 sales@wuyanpharm.com China 63 55
Shanghai Boyle Chemical Co., Ltd.
86-21-57758967 sales@boylechem.com China 2926 55
J & K SCIENTIFIC LTD. 400-666-7788 +86-10-82848833
86-10-82849933 jkinfo@jkchemical.com;market6@jkchemical.com China 96815 76

View Lastest Price from MK-0822 manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2018-08-21 MK-0822
603139-19-1
US $1.00 / KG 1G 98% 100KG career henan chemical co

603139-19-1(MK-0822)Related Search:


  • (2S)-N-(1-cyanocyclopropyl)-4-fluoro-4-Methyl-2-{[(1S)-2,2,2-trifluoro-1-[4-(4-Methanesulfonylphenyl)phenyl]ethyl]aMino}pentanaMide
  • (2S)-N-(1-cyanocyclopropyl)-4-fluoro-4-methyl-2-[[(1S)-2,2,2-trifluoro-1-[4-(4-methylsulfonylphenyl)phenyl]ethyl]amino]pentanamide
  • (MK0822,Odanacatib)
  • Odanacatib,MK-0822,MK0822
  • Pentanamide, N-(1-cyanocyclopropyl)-4-fluoro-4-methyl-2-[[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)[1,1'-biphenyl]-4-yl]ethyl]amino]-, (2S)-
  • (2S)-N-(1-Cyanocyclopropyl)-4-fluoro-4-methyl-2-[[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)[1,1'-biphenyl]-4-yl]ethyl]amino]pentanamide Odanacatib (MK-0822)
  • Odanacatib (2S)-N-(1-Cyanocyclopropyl)-4-fluoro-4-methyl-2-[[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)[1,1'-biphenyl]-4-yl]ethyl]amino]pentanamide
  • (S)-N-(1-cyanocyclopropyl)-4-fluoro-4-methyl-2-((S)-2,2,2-trifluoro-1-(4'-(methylsulfonyl)biphenyl-4-yl)ethylamino)pentanamide
  • Odanacatib, >=98%
  • MK-0822
  • ODANACATIB
  • (2S)-N-(1-Cyanocyclopropyl)-4-fluoro-4-methyl-2-[[(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)[1,1'-biphenyl]-4-yl]ethyl]amino]pentanamide
  • Unii-N673F6W2vh
  • N-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4'-(methylsulfonyl)biphenyl-4-yl]ethyl}-L-leucinamide
  • Odanacatib(Mk0822)
  • (S)-N-(1-cyanocyclopropyl)-4-fluoro-4-Methyl-2-(((S)-2,2,2-trifluoro-1-(4'-(Methylsulfonyl)-[1,1'-biphenyl]-4-yl)ethyl)aMino)pentanaMide
  • 603139-19-1
  • C25H27F4N3O3S
  • API
  • Inhibitors
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