1. GPCR/G Protein
  2. Protease Activated Receptor (PAR)
  3. UDM-001651

UDM-001651 is a potent, selective, and orally bioavailable protease-activated receptor 4 (PAR4) antagonist (IC50=4 nM; Kd=1.4 nM). UDM-001651 shows antiplatelet potency (IC50=25 nM) in a γ-thrombin-induced platelet-rich plasma aggregation assay (γ-Thr PRP).

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UDM-001651

UDM-001651 화학구조

CAS No. : 1477497-01-0

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제품 설명

UDM-001651 is a potent, selective, and orally bioavailable protease-activated receptor 4 (PAR4) antagonist (IC50=4 nM; Kd=1.4 nM). UDM-001651 shows antiplatelet potency (IC50=25 nM) in a γ-thrombin-induced platelet-rich plasma aggregation assay (γ-Thr PRP)[1].

IC50 & Target

PAR4

 

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
2.4 nM
Compound: 54; UDM-001651
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
Antagonist activity at full-length human PAR4 expressed in HEK293 cells assessed as inhibition of AYPGKF-induced intracellular calcium mobilization preincubated for 30 mins followed by AYPGKF addition and measured by calcium indicator-based FLIPR assay
[PMID: 31246024]
Platelet IC50
25 nM
Compound: 1; UDM-00165
Antiplatelet activity in human platelet-rich plasma assessed as inhibition of gamma thrombin induced platelet aggregation preincubated for 5 mins followed by gamma thrombin addition and measured upto 15 mins by plate reader assay
Antiplatelet activity in human platelet-rich plasma assessed as inhibition of gamma thrombin induced platelet aggregation preincubated for 5 mins followed by gamma thrombin addition and measured upto 15 mins by plate reader assay
[PMID: 35729784]
분자량

513.56

화학식

C28H23N3O5S

CAS No.
SMILES

COC1=CC(OCC2=CC=CC(OCC3=CC=CC=C3)=C2)=C4C=C(C5=CN6C(SC(OC)=N6)=N5)OC4=C1

선적

Room temperature in continental US; may vary elsewhere.

보관

Please store the product under the recommended conditions in the Certificate of Analysis.

순도&문서
References
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Inquiry Information

상품명:
UDM-001651
Cat. No.:
HY-128345
수량:
MCE Japan Authorized Agent: