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1174850-85-1

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1174850-85-1 Usage

Check Digit Verification of cas no

The CAS Registry Mumber 1174850-85-1 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,1,7,4,8,5 and 0 respectively; the second part has 2 digits, 8 and 5 respectively.
Calculate Digit Verification of CAS Registry Number 1174850-85:
(9*1)+(8*1)+(7*7)+(6*4)+(5*8)+(4*5)+(3*0)+(2*8)+(1*5)=171
171 % 10 = 1
So 1174850-85-1 is a valid CAS Registry Number.

1174850-85-1Downstream Products

1174850-85-1Relevant articles and documents

Improvement of Oral Bioavailability of Pyrazolo-Pyridone Inhibitors of the Interaction of DCN1/2 and UBE2M

Kim, Ho Shin,Hammill, Jared T.,Scott, Daniel C.,Chen, Yizhe,Rice, Amy L.,Pistel, William,Singh, Bhuvanesh,Schulman, Brenda A.,Guy, R. Kiplin

supporting information, p. 5850 - 5862 (2021/05/29)

The cullin-RING ubiquitin ligases (CRLs) are ubiquitin E3 enzymes that play a key role in controlling proteasomal degradation and are activated by neddylation. We previously reported inhibitors that target CRL activation by disrupting the interaction of defective in cullin neddylation 1 (DCN1), a CRL neddylation co-E3, and UBE2M, a neddylation E2. Our first-generation inhibitors possessed poor oral bioavailability and fairly rapid clearance that hindered the study of acute inhibition of DCN-controlled CRL activity in vivo. Herein, we report studies to improve the pharmacokinetic performance of the pyrazolo-pyridone inhibitors. The current best inhibitor, 40, inhibits the interaction of DCN1 and UBE2M, blocks NEDD8 transfer in biochemical assays, thermally stabilizes cellular DCN1, and inhibits anchorage-independent growth in a DCN1 amplified squamous cell carcinoma cell line. Additionally, we demonstrate that a single oral 50 mg/kg dose sustains plasma exposures above the biochemical IC90 for 24 h in mice.

Discovery and Characterization of 1H-Pyrazol-5-yl-2-phenylacetamides as Novel, Non-Urea-Containing GIRK1/2 Potassium Channel Activators

Wieting, Joshua M.,Vadukoot, Anish K.,Sharma, Swagat,Abney, Kristopher K.,Bridges, Thomas M.,Daniels, J. Scott,Morrison, Ryan D.,Wickman, Kevin,Weaver, C. David,Hopkins, Corey R.

, p. 1873 - 1879 (2017/09/25)

The G protein-gated inwardly-rectifying potassium channels (GIRK, Kir3) are a family of inward-rectifying potassium channels, and there is significant evidence supporting the roles of GIRKs in a number of physiological processes and as potential targets for numerous indications. Previously reported urea containing molecules as GIRK1/2 preferring activators have had significant pharmacokinetic (PK) liabilities. Here we report a novel series of 1H-pyrazolo-5-yl-2-phenylacetamides in an effort to improve upon the PK properties. This series of compounds display nanomolar potency as GIRK1/2 activators with improved brain distribution (rodent Kp > 0.6).

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