RO-5006036


Catalog No. size PriceQuantity
M7068-2 2mg solid $138
M7068-10 10mg solid $556

Description

Cas:939375-07-2

Product Information

RO-5006036, also known as DGAT1-IN-3, is a potent, selective and orally bioavailable inhibitor of DGAT-1.

 

Chemical Formula: C20H19F3N4O3

 

Exact Mass: 420.1409

 

Molecular Weight: 420.3922

 

Elemental Analysis: C, 57.14; H, 4.56; F, 13.56; N, 13.33; O, 11.42

 

Synonym:

DGAT1-IN-3

RO-5006036

RO 5006036

RO5006036

 

Chemical Name: N-(6-((2-methoxyethyl)(methyl)amino)pyridin-3-yl)-2-phenyl-5-(trifluoromethyl)oxazole-4-carboxamide

 

InChi Key: 

QEZWDFXCTTZZRI-UHFFFAOYSA-N

 

InChi Code: InChI=1S/C20H19F3N4O3/c1-27(10-11-29-2)15-9-8-14(12-24-15)25-18(28)16-17(20(21,22)23)30-19(26-16)13-6-4-3-5-7-13/h3-9,12H,10-11H2,1-2H3,(H,25,28)

 

Smiles Code:

O=C(C1=C(C(F)(F)F)OC(C2=CC=CC=C2)=N1)NC3=CC=C(N(CCOC)C)N=C3

 

 

Technical Data:

 

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

Shelf Life: >3 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

 

In Vitro:

DGAT1-IN-3 blocks the human ether-a-go-go-related gene (hERG) encoded potassium channel with an IC20 of 0.2 μM.

DGAT1-IN-3 inhibits human DGAT-1 in CHOK1 cells with an EC50 of 0.66 μM.

 

In Vivo:

DGAT1-IN-3 (5-50 mg/kg; p.o once daily for three weeks) reduces weight gain and plasma triglycerides, and improves lipid profile.

DGAT1-IN-3 (50 mg/kg; p.o) exhibits good oral bioavailability (77%) and the maximum exposure level in plasma (Cmax) is 24 μM.

DGAT1-IN-3 (5 mg/kg; i.v) exhibits terminal elimination half-lives (1.95 h) and low clearance (13.5 mL/min/kg).

 

 

References

 

  1. Yimin Q, et, al. Discovery of orally active carboxylic acid derivatives of 2-phenyl-5-trifluoromethyloxazole-4-carboxamide as potent diacylglycerol acyltransferase-1 inhibitors for the potential treatment of obesity and diabetes. J Med Chem. 2011 Apr 14; 54(7): 2433-46.

 

  1. Weiya Y, et, al. Discovery and optimization of 2-phenyloxazole derivatives as diacylglycerol acyltransferase-1 inhibitors. Bioorg Med Chem Lett. 2011 Dec 1; 21(23): 7205-9.

 

Products are for research use only. Not for human use.

 

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