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

China 131 India 3 United Kingdom 2 United States 22 Global 158

LGM Pharma

Tel: 1-(800)-881-8210
Fax: 615-250-9817
Email: inquiries@lgmpharma.com
Country: United States
ProdList: 2127
Advantage: 70

AdooQ BioScience, LLC

Tel: +1 (866) 930-6790
Fax: +1 (866) 333-9607
Email: info@adooq.com
Country: United States
ProdList: 2784
Advantage: 58

Target molecule Corp.

Tel: 857-239-0968
Fax: 857-239-8801
Email: service1@targetmol.com
Country: United States
ProdList: 2559
Advantage: 60

Alabiotech Inc.

Tel: 001-619-354-5251
Fax: 001-855-855-6087
Email: sales@alabiotech-e.com
Country: United States
ProdList: 972
Advantage: 60

Musechem

Tel: +1-800-259-7612
Fax: +1-800-259-7612
Email: info@musechem.com
Country: United States
ProdList: 4662
Advantage: 60

InvivoChem

Tel: +1-708-310-1919 +1-13798911105
Fax: 708-557-7486
Email: sales@invivochem.cn
Country: United States
ProdList: 6393
Advantage: 58

Cckinase, Inc.

Tel: +1 (732)236-3202
Email: sales@cckinase.com
Country: United States
ProdList: 2738
Advantage: 58

BOC Sciences

Tel: +1-631-485-4226
Fax: 1-631-614-7828
Email: inquiry@bocsci.com
Country: United States
ProdList: 19553
Advantage: 58

Aladdin Scientific

Tel: +1-833-552-7181
Email: sales@aladdinsci.com
Country: United States
ProdList: 57511
Advantage: 58

TargetMol Chemicals Inc.

Tel: +1-781-999-5354
Email: support@targetmol.com
Country: United States
ProdList: 19973
Advantage: 58

Aceschem Inc.

Tel: +1-817863-6948 +1-（817）863-6948
Email: sales@aceschem.com
Country: United States
ProdList: 19639
Advantage: 58

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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:

Cyanoacetic acid Benzonitrile 5'-D(ATGAAAATCAGGGTTAGG)-3', SODIUM SALT PD168393 MK-1775 Saracatinib Ibrutinib Olaparib Pentanamide N-(2-(BENZYLAMINO)ETHYL) CYCLOPROPANAMINE Odanacatib (MK-0822)

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