Product Name :
MK-0812 Succinate
Description:
MK-0812 Succinate is a potent and selective CCR2 antagonist with high affinity at CCR2.
CAS:
851916-42-2
Molecular Weight:
587.63
Formula:
C28H40F3N3O7
Chemical Name:
(3S,4S)-3-methoxy-N-[(1R,3S)-3-(propan-2-yl)-3-[3-(trifluoromethyl)-5,6,7,8-tetrahydro-1,6-naphthyridine-6-carbonyl]cyclopentyl]oxan-4-amine; butanedioic acid
Smiles :
CC(C)[C@]1(C[C@@H](CC1)N[C@H]1CCOC[C@H]1OC)C(=O)N1CC2=CC(=CN=C2CC1)C(F)(F)F.OC(=O)CCC(O)=O
InChiKey:
WPPJJJUIDYHHSM-PXUYIWLPSA-N
InChi :
InChI=1S/C24H34F3N3O3.C4H6O4/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;5-3(6)1-2-4(7)8/h10,12,15,18,20-21,29H,4-9,11,13-14H2,1-3H3;1-2H2,(H,5,6)(H,7,8)/t18-,20+,21-,23+;/m1.{{Allopurinol} MedChemExpress|{Allopurinol} Xanthine Oxidase|{Allopurinol} Purity & Documentation|{Allopurinol} References|{Allopurinol} custom synthesis|{Allopurinol} Autophagy} /s1
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
MK-0812 Succinate is a potent and selective CCR2 antagonist with high affinity at CCR2.|Product information|CAS Number: 851916-42-2|Molecular Weight: 587.63|Formula: C28H40F3N3O7|Chemical Name: (3S,4S)-3-methoxy-N-[(1R,3S)-3-(propan-2-yl)-3-[3-(trifluoromethyl)-5,6,7,8-tetrahydro-1,6-naphthyridine-6-carbonyl]cyclopentyl]oxan-4-amine; butanedioic acid|Smiles: CC(C)[C@]1(C[C@@H](CC1)N[C@H]1CCOC[C@H]1OC)C(=O)N1CC2=CC(=CN=C2CC1)C(F)(F)F.OC(=O)CCC(O)=O|InChiKey: WPPJJJUIDYHHSM-PXUYIWLPSA-N|InChi: InChI=1S/C24H34F3N3O3.C4H6O4/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;5-3(6)1-2-4(7)8/h10,12,15,18,20-21,29H,4-9,11,13-14H2,1-3H3;1-2H2,(H,5,6)(H,7,8)/t18-,20+,21-,23+;/m1./s1|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO : ≥ 32 mg/mL (54.46 mM).|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.{{Sincalide} medchemexpress|{Sincalide} Akt|{Sincalide} Biological Activity|{Sincalide} In Vitro|{Sincalide} supplier|{Sincalide} Epigenetics} |Shelf Life: ≥12 months if stored properly.PMID:24733396 |Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|MK-0812 is a potent and selective CCR2 antagonist. MK-0812 completely blocks all MCP-1 mediated response in a concentration dependent manner, with an IC50 of 3.2 nM. This value is similar to the potency observed for the inhibition of 125I-MCP-1 binding by MK-0812 on isolated monocytes (IC50 4.5 nM). In fact, MK-0812 not only completely blocks the shape change response to exogenous MCP-1, but also results in a monocyte forward scatter measurement below unstimulated or basal levels. The addition of MK-0812 to rhesus blood also inhibits MCP-1 induced monocyte shape change. The IC50 for MK-0812 in whole blood assays is 8 nM|In Vivo:|MK-0812 (30 mg/kg, p.o.) reduces the frequency of Ly6G-Ly6Chi monocytes in the peripheral blood, while no impact on circulating Ly6G+Ly6C+ neutrophil frequency is observed. In addition, MK-0812 treatment causes a dose-dependent reduction in circulating Ly6Chi monocytes and a corresponding elevation in the CCR2 ligand CCL2. MK-0812 is administered by continuous i.v. infusion to maintain a constant level of the drug in blood.|Products are for research use only. Not for human use.|
