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MedKoo Cat#: 522494 | Name: AZD-7687

Description:

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

AZD7687, a reversible and selective DGAT1 inhibitor with IC50 value of 80 nM. AZD-7687 attenuates postprandial triacylglyceride excursion. AZD7687 markedly reduced postprandial TAG excursion with a steep concentration-effect relationship. Incremental TAG AUC (area under the serum concentration vs. time curve) following SMM 60% was decreased >75% from baseline at doses ≥5 mg (p < 0.0001 vs. placebo). Serum levels of diacylglycerol, specifically measured with mass spectrometry, did not increase after AZD7687 administration. Nausea, vomiting and diarrhoea were reported with increasing doses and they limited dose escalation. Lowering of SMM fat content to 45 or 30% in five cohorts gradually reduced the frequency of gastrointestinal symptoms at a given dose of AZD7687.

Chemical Structure

AZD-7687
AZD-7687
CAS#1166827-44-6

Theoretical Analysis

MedKoo Cat#: 522494

Name: AZD-7687

CAS#: 1166827-44-6

Chemical Formula: C21H25N3O3

Exact Mass: 367.1896

Molecular Weight: 367.45

Elemental Analysis: C, 68.64; H, 6.86; N, 11.44; O, 13.06

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
No Data
Synonym
AZD-7687; AZD 7687; AZD7687.
IUPAC/Chemical Name
2-((1s,4s)-4-(4-(6-carbamoyl-3,5-dimethylpyrazin-2-yl)phenyl)cyclohexyl)acetic acid
InChi Key
YXFNPRHZMOGREC-GASCZTMLSA-N
InChi Code
InChI=1S/C21H25N3O3/c1-12-19(24-20(21(22)27)13(2)23-12)17-9-7-16(8-10-17)15-5-3-14(4-6-15)11-18(25)26/h7-10,14-15H,3-6,11H2,1-2H3,(H2,22,27)(H,25,26)/t14-,15+
SMILES Code
OC(C[C@H]1CC[C@@H](C2=CC=C(C3=C(C)N=C(C(C(N)=O)=N3)C)C=C2)CC1)=O
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
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 367.45 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.

Recalculate based on batch purity %
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
1: Floettmann E, Lees D, Seeliger F, Jones HB. Pharmacological inhibition of DGAT1 induces sebaceous gland atrophy in mouse and dog skin while overt alopecia is restricted to the mouse. Toxicol Pathol. 2015 Apr;43(3):376-83. doi: 10.1177/0192623314545657. Epub 2014 Aug 11. PubMed PMID: 25112279. 2: Denison H, Nilsson C, Löfgren L, Himmelmann A, Mårtensson G, Knutsson M, Al-Shurbaji A, Tornqvist H, Eriksson JW. Diacylglycerol acyltransferase 1 inhibition with AZD7687 alters lipid handling and hormone secretion in the gut with intolerable side effects: a randomized clinical trial. Diabetes Obes Metab. 2014 Apr;16(4):334-43. doi: 10.1111/dom.12221. Epub 2013 Oct 31. PubMed PMID: 24118885. 3: Barlind JG, Bauer UA, Birch AM, Birtles S, Buckett LK, Butlin RJ, Davies RD, Eriksson JW, Hammond CD, Hovland R, Johannesson P, Johansson MJ, Kemmitt PD, Lindmark BT, Morentin Gutierrez P, Noeske TA, Nordin A, O'Donnell CJ, Petersson AU, Redzic A, Turnbull AV, Vinblad J. Design and optimization of pyrazinecarboxamide-based inhibitors of diacylglycerol acyltransferase 1 (DGAT1) leading to a clinical candidate dimethylpyrazinecarboxamide phenylcyclohexylacetic acid (AZD7687). J Med Chem. 2012 Dec 13;55(23):10610-29. doi: 10.1021/jm301296t. Epub 2012 Nov 21. PubMed PMID: 23116186. 4: Denison H, Nilsson C, Kujacic M, Löfgren L, Karlsson C, Knutsson M, Eriksson JW. Proof of mechanism for the DGAT1 inhibitor AZD7687: results from a first-time-in-human single-dose study. Diabetes Obes Metab. 2013 Feb;15(2):136-43. doi: 10.1111/dom.12002. Epub 2012 Sep 30. PubMed PMID: 22950654.