MedKoo Cat#: 555134 | Name: AS2553627

Description:

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

AS2553627 is a novel JAK inhibitor. AS2553627 prevents chronic rejection in rat cardiac allografts. AS2553627 potently inhibited JAK kinases but showed no inhibition of other kinases, including TCR-associated molecules. In a rat cardiac transplant model, oral administration of AS2553627 alone or co-administration with a sub-therapeutic dose of tacrolimus effectively prolonged cardiac allograft survival, suggesting the efficacy in treating acute rejection. AS2553627 may be a therapeutic candidate for the prevention of not only acute but also chronic rejection in cardiac transplantation.

Chemical Structure

AS2553627
CAS#1251906-10-1

Theoretical Analysis

MedKoo Cat#: 555134

Name: AS2553627

CAS#: 1251906-10-1

Chemical Formula: C18H19N5O

Exact Mass: 321.1590

Molecular Weight: 321.38

Elemental Analysis: C, 67.27; H, 5.96; N, 21.79; O, 4.98

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
AS2553627; AS-2553627; AS 2553627.
IUPAC/Chemical Name
3-((3R,4R)-3-(dipyrrolo[2,3-b:2',3'-d]pyridin-1(6H)-yl)-4-methylpiperidin-1-yl)-3-oxopropanenitrile
InChi Key
UQVAOELSLJXOMB-DOMZBBRYSA-N
InChi Code
InChI=1S/C18H19N5O/c1-12-4-8-22(16(24)2-6-19)11-15(12)23-9-5-13-10-21-18-14(17(13)23)3-7-20-18/h3,5,7,9-10,12,15H,2,4,8,11H2,1H3,(H,20,21)/t12-,15+/m1/s1
SMILES Code
N#CCC(N1C[C@H](N2C=CC3=CN=C(NC=C4)C4=C32)[C@H](C)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
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
Janus family kinases (JAKs) are essential molecules for cytokine responses and attractive targets for the treatment of transplant rejection and autoimmune diseases. Several JAK inhibitors have shown demonstrable effects on acute rejection in experimental cardiac transplant models. AS2553627 significantly reduced cardiac allograft vasculopathy and fibrosis that tacrolimus alone did not inhibit. AS2553627 at the effective dose in rat transplantation models did not significantly reduce reticulocyte counts in peripheral whole blood after in vivo erythropoietin administration, indicating a low risk for anemia.

Preparing Stock Solutions

The following data is based on the product molecular weight 321.38 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: Nakamura K, Inami M, Morio H, Okuma K, Ito M, Noto T, Shirakami S, Hirose J, Morokata T. AS2553627, a novel JAK inhibitor, prevents chronic rejection in rat cardiac allografts. Eur J Pharmacol. 2017 Feb 5;796:69-75. doi: 10.1016/j.ejphar.2016.12.025. Epub 2016 Dec 16. PubMed PMID: 27993641.