| Field | Specification |
|---|---|
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C22H26N6O6S |
| SMILES | |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
CRL-42872 free base is an orally active, highly bioavailable Gp IIb/IIIa platelet receptor inhibitor. It inhibits the binding of fibrinogen to the Gp IIb/IIIa receptor, thereby suppressing collagen-induced platelet aggregation, and it is used in thrombosis-related studies[1]. It has the molecular formula C22H26N6O6S and a molecular weight of 502.54 g/mol.
Physical & Chemical Properties
| CAS Number | 256344-23-7 |
|---|---|
| Molecular Formula | C22H26N6O6S |
| Molecular Weight | 502.54 g/mol |
| SMILES | O=C1CN(C2=CC=C(C=C2)C(N)=N)CCN1CC(NC[C@@H](C(O)=O)NS(=O)(C3=CC=CC=C3)=O)=O |
| Signaling Pathway | Membrane Transporter/Ion Channel |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
[1]. Yue C, et al. Substituted piperazinones and their therapeutic uses: U.S. Patent 6,335,337[P]. 2002-1-1.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with your institution's chemical hygiene plan.
In Vitro
CRL-42872 free base (1.5×10-8 M - 7×10-5 M; 3 minutes) is a potent inhibitor of collagen-induced aggregation of guinea pig platelets, with an IC50 of 9.4×10-8 M[1]. In human platelets, CRL-42872 free base (10-8 M - 5×10-5 M; 3 minutes) also inhibits collagen-induced aggregation, with an IC50 of 1.2×10-7 M[1].
In Vivo
A single oral dose of CRL-42872 free base (10 mg/kg; p.o.) inhibits collagen-induced guinea pig platelet aggregation[1].
| Animal Model | Dunkin-Hartley (male, ~330 g)[1] |
|---|---|
| Dosage | 10 mg/kg |
| Administration | p.o.; single dose |
| Result | Inhibited collagen-induced platelet aggregation by 68% at 1 hour post-administration. Inhibited collagen-induced platelet aggregation by 64% at 2 hours post-administration. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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