MK 0812 | CAS#624733-88-6 | CCR2 antagonist

MedKoo Cat#: 525674 | Name: MK-0812

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

MK-0812 is a potent and selective CCR2 antagonist. Chemokine (C-C motif) receptor 2 (CCR2) is central for the migration of monocytes into inflamed tissues. The inhibition of CCR2 signaling represents a potential therapeutic approach for treatment of metastasis without affecting homeostatic functions.

Chemical Structure

MK-0812

CAS#624733-88-6

Theoretical Analysis

MedKoo Cat#: 525674

Name: MK-0812

CAS#: 624733-88-6

Chemical Formula: C24H34F3N3O3

Exact Mass: 469.2552

Molecular Weight: 469.55

Elemental Analysis: C, 61.39; H, 7.30; F, 12.14; N, 8.95; O, 10.22

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 385.00	2 Weeks
10mg	USD 715.00	2 Weeks

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Related CAS #

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Synonym

MK-0812; MK 0812; MK0812.

IUPAC/Chemical Name

((1S,3R)-1-isopropyl-3-(((3S,4S)-3-methoxytetrahydro-2H-pyran-4-yl)amino)cyclopentyl)(3-(trifluoromethyl)-7,8-dihydro-1,6-naphthyridin-6(5H)-yl)methanone

InChi Key

MTMDXAIUENDNDL-RJSMDTJLSA-N

InChi Code

InChI=1S/C24H34F3N3O3/c1-15(2)23(7-4-18(11-23)29-20-6-9-33-14-21(20)32-3)22(31)30-8-5-19-16(13-30)10-17(12-28-19)24(25,26)27/h10,12,15,18,20-21,29H,4-9,11,13-14H2,1-3H3/t18-,20+,21-,23+/m1/s1

SMILES Code

CC(C)[C@@]1(CC[C@H](C1)N[C@H]2CCOC[C@H]2OC)C(=O)N3CCC4=NC=C(C=C4C3)C(F)(F)F

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO, not in water

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

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Product Data

Product Data

Instruction

View handling instruction

Biological target:

MK-0812 is a potent and selective CCR2 antagonist with low nM affinity for CCR2.

In vitro activity:

TBD

In vivo activity:

This study explored the effects of small molecule chemokine receptor antagonists to block migration of these cells in anti-collagen antibody-induced arthritis mouse model. MK0812 selectively reduced the peripheral blood monocyte frequency, and caused an elevation in the CCR2 ligand CCL2. Reference: Biochem Biophys Res Commun. 2010 Jan 1;391(1):1080-6. https://pubmed.ncbi.nlm.nih.gov/20004647/

	Solvent	mg/mL	mM
Solubility
	DMF	15.0	31.95
	DMF:PBS (pH 7.2) (1:20)	0.0	0.09
	DMSO	1.0	2.13
	Ethanol	10.0	21.30

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 469.55 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. O'Brien PD, Hinder LM, Parlee SD, Hayes JM, Backus C, Zhang H, Ma L, Sakowski SA, Brosius FC 3rd, Feldman EL. Dual CCR2/CCR5 antagonist treatment attenuates adipose inflammation, but not microvascular complications in ob/ob mice. Diabetes Obes Metab. 2017 Oct;19(10):1468-1472. doi: 10.1111/dom.12950. Epub 2017 Jun 2. PMID: 28332276; PMCID: PMC5610585. 2. Min SH, Wang Y, Gonsiorek W, Anilkumar G, Kozlowski J, Lundell D, Fine JS, Grant EP. Pharmacological targeting reveals distinct roles for CXCR2/CXCR1 and CCR2 in a mouse model of arthritis. Biochem Biophys Res Commun. 2010 Jan 1;391(1):1080-6. doi: 10.1016/j.bbrc.2009.12.025. Epub 2009 Dec 14. PMID: 20004647.

In vitro protocol:

TBD

In vivo protocol:

1: Wisniewski T, Bayne E, Flanagan J, Shao Q, Wnek R, Matheravidathu S, Fischer P, Forrest MJ, Peterson L, Song X, Yang L, Demartino JA, Struthers M. Assessment of chemokine receptor function on monocytes in whole blood: In vitro and ex vivo evaluations of a CCR2 antagonist. J Immunol Methods. 2010 Jan 31;352(1-2):101-10. doi: 10.1016/j.jim.2009.10.010. Epub 2009 Nov 10. PubMed PMID: 19913021. 1: Min SH, Wang Y, Gonsiorek W, Anilkumar G, Kozlowski J, Lundell D, Fine JS, Grant EP. Pharmacological targeting reveals distinct roles for CXCR2/CXCR1 and CCR2 in a mouse model of arthritis. Biochem Biophys Res Commun. 2010 Jan 1;391(1):1080-6. doi: 10.1016/j.bbrc.2009.12.025. Epub 2009 Dec 14. PubMed PMID: 20004647.