AZD7545
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MedKoo CAT#: 530493

CAS#: 252017-04-2

Description: AZD7545 is an inhibitor of pyruvate dehydrogenase kinase 2 (PDHK2) (IC50 value of 6.4nM ) for the treatment of type 2 diabetes. AZD7545 activates pyruvate dehydrogenase in vivo and improves blood glucose control in obese (fa/fa) Zucker rats.


Price and Availability

Size Price Shipping out time Quantity
10mg USD 190 2 Weeks
25mg USD 420 2 Weeks
50mg USD 750 2 Weeks
100mg USD 1350 2 Weeks
200mg USD 1950 2 Weeks
500mg USD 2650 2 Weeks
1g USD 3850 2 Weeks
2g USD 6450 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2020-10-24. Prices are subject to change without notice.

AZD7545, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 530493
Name: AZD7545
CAS#: 252017-04-2
Chemical Formula: C19H18ClF3N2O5S
Exact Mass: 478.0577
Molecular Weight: 478.8672
Elemental Analysis: C, 47.66; H, 3.79; Cl, 7.40; F, 11.90; N, 5.85; O, 16.71; S, 6.69


Synonym: AZD7545; AZD-7545; AZD 7545.

IUPAC/Chemical Name: 4-[3-chloro-4-[[(2R)-3,3,3-trifluoro-2-hydroxy-2-methylpropanoyl]amino]phenyl]sulfonyl-N,N-dimethylbenzamide

InChi Key: DTDZLJHKVNTQGZ-GOSISDBHSA-N

InChi Code: InChI=1S/C19H18ClF3N2O5S/c1-18(28,19(21,22)23)17(27)24-15-9-8-13(10-14(15)20)31(29,30)12-6-4-11(5-7-12)16(26)25(2)3/h4-10,28H,1-3H3,(H,24,27)/t18-/m1/s1

SMILES Code: O=C(N(C)C)C1=CC=C(S(=O)(C2=CC=C(NC([C@@](C)(O)C(F)(F)F)=O)C(Cl)=C2)=O)C=C1


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:
>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


References

1: Kato M, Li J, Chuang JL, Chuang DT. Distinct structural mechanisms for inhibition of pyruvate dehydrogenase kinase isoforms by AZD7545, dichloroacetate, and radicicol. Structure. 2007 Aug;15(8):992-1004. PubMed PMID: 17683942; PubMed Central PMCID: PMC2871385.

2: Tuganova A, Klyuyeva A, Popov KM. Recognition of the inner lipoyl-bearing domain of dihydrolipoyl transacetylase and of the blood glucose-lowering compound AZD7545 by pyruvate dehydrogenase kinase 2. Biochemistry. 2007 Jul 24;46(29):8592-602. PubMed PMID: 17602666; PubMed Central PMCID: PMC2136408.

3: Mayers RM, Butlin RJ, Kilgour E, Leighton B, Martin D, Myatt J, Orme JP, Holloway BR. AZD7545, a novel inhibitor of pyruvate dehydrogenase kinase 2 (PDHK2), activates pyruvate dehydrogenase in vivo and improves blood glucose control in obese (fa/fa) Zucker rats. Biochem Soc Trans. 2003 Dec;31(Pt 6):1165-7. Review. PubMed PMID: 14641018.

4: Morrell JA, Orme J, Butlin RJ, Roche TE, Mayers RM, Kilgour E. AZD7545 is a selective inhibitor of pyruvate dehydrogenase kinase 2. Biochem Soc Trans. 2003 Dec;31(Pt 6):1168-70. PubMed PMID: 14641019.

5: Makita N, Ishiguro J, Suzuki K, Nara F. Dichloroacetate induces regulatory T-cell differentiation and suppresses Th17-cell differentiation by pyruvate dehydrogenase kinase-independent mechanism. J Pharm Pharmacol. 2017 Jan;69(1):43-51. doi: 10.1111/jphp.12655. PubMed PMID: 27757958.

6: Jones HB, Reens J, Johnson E, Brocklehurst S, Slater I. Myocardial steatosis and necrosis in atria and ventricles of rats given pyruvate dehydrogenase kinase inhibitors. Toxicol Pathol. 2014 Dec;42(8):1250-66. doi: 10.1177/0192623314530195. PubMed PMID: 24742628.

7: Hiromasa Y, Yan X, Roche TE. Specific ion influences on self-association of pyruvate dehydrogenase kinase isoform 2 (PDHK2), binding of PDHK2 to the L2 lipoyl domain, and effects of the lipoyl group-binding site inhibitor, Nov3r. Biochemistry. 2008 Feb 26;47(8):2312-24. doi: 10.1021/bi7014772. PubMed PMID: 18220415.

8: Li J, Kato M, Chuang DT. Pivotal role of the C-terminal DW-motif in mediating inhibition of pyruvate dehydrogenase kinase 2 by dichloroacetate. J Biol Chem. 2009 Dec 4;284(49):34458-67. doi: 10.1074/jbc.M109.065557. PubMed PMID: 19833728; PubMed Central PMCID: PMC2797213.

9: Wynn RM, Kato M, Chuang JL, Tso SC, Li J, Chuang DT. Pyruvate dehydrogenase kinase-4 structures reveal a metastable open conformation fostering robust core-free basal activity. J Biol Chem. 2008 Sep 12;283(37):25305-15. doi: 10.1074/jbc.M802249200. PubMed PMID: 18658136; PubMed Central PMCID: PMC2533096.

10: Mayers RM, Leighton B, Kilgour E. PDH kinase inhibitors: a novel therapy for Type II diabetes? Biochem Soc Trans. 2005 Apr;33(Pt 2):367-70. Review. PubMed PMID: 15787608.