Bioactivity In vitro In vivo Features
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MK-0822

Bioactivity In vitro In vivo Features
Product Name
MK-0822
CAS No.
603139-19-1
Chemical Name
MK-0822
Synonyms
CS-700;MK-0822;ODANACATIB;MK-0822;MK0822;Unii-N673F6W2vh;Odanacatib, >=98%;Odanacatib(Mk0822);(MK0822,Odanacatib);Odanacatib,MK-0822,MK0822;Pentanamide,N-(1-cyanocyclopropyl)-4-fluoro-4-methyl-2-[[(1S...
CBNumber
CB52455399
Molecular Formula
C25H27F4N3O3S
Formula Weight
525.56
MOL File
603139-19-1.mol
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MK-0822 Property

Melting point:
223-224 °C
Boiling point:
681.6±55.0 °C(Predicted)
Density 
1.35
storage temp. 
Sealed in dry,Store in freezer, under -20°C
solubility 
Chloroform (Slightly, Heated, Sonicated), Methanol (Slightly, Sonicated)
form 
Solid
pka
12.06±0.20(Predicted)
color 
White to Off-White
Stability:
Hygroscopic
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Danger
Hazard statements

H373May cause damage to organs through prolonged or repeated exposure

Precautionary statements

P260Do not breathe dust/fume/gas/mist/vapours/spray.

P314Get medical advice/attention if you feel unwell.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical
Product number
21466
Product name
Odanacatib
Purity
≥98%
Packaging
1mg
Price
$57
Updated
2024/03/01
Cayman Chemical
Product number
21466
Product name
Odanacatib
Purity
≥98%
Packaging
5mg
Price
$233
Updated
2024/03/01
Cayman Chemical
Product number
21466
Product name
Odanacatib
Purity
≥98%
Packaging
10mg
Price
$437
Updated
2024/03/01
Cayman Chemical
Product number
21466
Product name
Odanacatib
Purity
≥98%
Packaging
25mg
Price
$957
Updated
2024/03/01
TRC
Product number
M425015
Product name
MK-0822
Packaging
100mg
Price
$770
Updated
2021/12/16
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MK-0822 Chemical Properties,Usage,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

Uses

MK-0822 is a newly developed bone-targeting dual action pro-drug for osteoporosis and bone metastasis. It is also an inhibitor of cathepsin K, an enzyme involved in bone resorption.

Biological Activity

odanacatib (mk-0822) is a potent, orally active and selective inhibitor of cathepsin k with ic50 value of 0.20 nm [1],cathepsin k is expressed predominantly in osteoclasts and degrades the collagen matrix componentsofbone. it plays a central role in mediating bone resorption. and the inhibitor of cathepsin k, odanacatib, is in development for the treatment of osteoporosis. based on preclinical evidence and available clinical data from dose-ranging phase iib trials, odanacatib appears to reduce bone resorptionwhile somewhat preserving bone formation in postmenopausalwomen. currently, odanacatib is undergoing evaluation for fracture risk reduction in a phase iii trial with >16000 patients with postmenopausal osteoporosis [2].chantal mahon, anish mehta, kate mostoller, stefan zajic, denise morris, jessie lee, and s. aubrey stoch. odanacatib, a selective cathepsin k inhibitor, demonstrates comparable pharmacodynamics and pharmacokinetics in older men and postmenopausal women. endocrine research. 2014, 99(2):552–560.

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.

target

cathepsin K

References

[1] s. aubrey stoch, stefan zajic, julie a. stone, deborah l. miller, lucas van bortel, kenneth c. lasseter, barnali pramanik, caroline cilissen, qi liu, lida liu, boyd b. scott, deborah panebianco, yu ding, keith gottesdiener & john a. wagner. odanacatib, a selective cathepsin k inhibitor to treat osteoporosis: safety, tolerability, pharmacokinetics and pharmacodynamics –results from single oral dose studies in healthy volunteers. british journal of clinical pharmacology. 2012, 75, (5): 1240-1254.
[2] matt s. anderson, isaias noel gendrano, chengcheng liu, steven jeffers,

MK-0822 Preparation Products And Raw materials

Raw materials

Preparation Products

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MK-0822 Suppliers

WuYan Pharmaceutical Technology (Shanghai) Co., Ltd.
Tel
021-61001086 13671938079
Fax
021-61114075
Email
sales@wuyanpharm.com
Country
China
ProdList
104
Advantage
55
Shanghai Boyle Chemical Co., Ltd.
Tel
Fax
86-21-57758967
Email
sales@boylechem.com
Country
China
ProdList
2922
Advantage
55
J & K SCIENTIFIC LTD.
Tel
010-82848833 400-666-7788
Fax
86-10-82849933
Email
jkinfo@jkchemical.com
Country
China
ProdList
94657
Advantage
76
Alabiochem Tech.Co., Ltd.
Tel
0512-58900862 400-0707518
Fax
0086-512-56765862
Email
sales@alabiochem.com
Country
China
ProdList
995
Advantage
59
Chembest Research Laboratories Limited
Tel
+86-21-20908456
Fax
021-58180499
Email
sales@BioChemBest.com
Country
China
ProdList
6005
Advantage
61
LGM Pharma
Tel
1-(800)-881-8210
Fax
615-250-9817
Email
inquiries@lgmpharma.com
Country
United States
ProdList
2123
Advantage
70
Shanghai Hanhong Scientific Co.,Ltd.
Tel
021-54306202 13764082696
Email
info@hanhongsci.com
Country
China
ProdList
42958
Advantage
64
Shanghai Feibo Chemical Technology Co., Ltd
Tel
021-58955608,2250286 15921236618
Email
blinkzeng@gmail.com
Country
China
ProdList
522
Advantage
62
Dalian Meilun Biotech Co., Ltd.
Tel
0411-62910999 13889544652
Email
meilunui@163.com
Country
China
ProdList
4727
Advantage
58
Anhui Shite Pharmaceutical Technology Co., LTD
Tel
0555-8228058 13621628489
Fax
0512-63261912
Email
sales1@stepuppharm.com
Country
China
ProdList
229
Advantage
55
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View Lastest Price from MK-0822 manufacturers

Henan Fengda Chemical Co., Ltd
Product
MK-0822 603139-19-1
Price
US $5.00-0.10/KG
Min. Order
1KG
Purity
98%
Supply Ability
g-kg-tons, free sample is available
Release date
2024-03-27
Zhuozhou Wenxi import and Export Co., Ltd
Product
Odanacatib 603139-19-1
Price
US $15.00-10.00/KG
Min. Order
1KG
Purity
99%+ HPLC
Supply Ability
Monthly supply of 1 ton
Release date
2021-07-10
Zhuozhou Wenxi import and Export Co., Ltd
Product
Odanacatib 603139-19-1
Price
US $15.00-10.00/KG
Min. Order
1KG
Purity
99%+ HPLC
Supply Ability
Monthly supply of 1 ton
Release date
2021-07-09

603139-19-1, MK-0822Related Search:


  • 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
  • CS-700
  • MK-0822;MK0822
  • (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)
  • Pentanamide,N-(1-cyanocyclopropyl)-4-fluoro-4-methyl-2-[[(1S...
  • (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