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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- CAS No.: 1477497-01-0
- 화학식: C28H23N3O5S
- 분자량:513.56
-
보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
|
PAR4 |
|
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] |
Chemical Information
-
CAS No. 1477497-01-0
-
분자량 513.56
-
화학식 C28H23N3O5S
-
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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)