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  4. Sibrafiban

Sibrafiban  (Synonyms: RO 48-3657)

Cat. No.: HY-10309 Purity: 99.67%
COA Handling Instructions

Sibrafiban (RO 48-3657) is the orally active, nonpeptide, double-prodrug of Ro 44-3888 and a selective glycoprotein IIb/IIIa receptor antagonist. Sibrafiban inhibits platelet aggregation.

For research use only. We do not sell to patients.

Sibrafiban Chemical Structure

Sibrafiban Chemical Structure

CAS No. : 172927-65-0

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Solution
10 mM * 1 mL in DMSO USD 330 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
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ready for reconstitution
 USD 330 In-stock
Estimated Time of Arrival: December 31
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5 mg USD 300 In-stock
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10 mg USD 480 In-stock
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25 mg USD 960 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1540 In-stock
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100 mg USD 2460 In-stock
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Description

Sibrafiban (RO 48-3657) is the orally active, nonpeptide, double-prodrug of Ro 44-3888 and a selective glycoprotein IIb/IIIa receptor antagonist. Sibrafiban inhibits platelet aggregation[1][2][3].

IC50 & Target

Glycoprotein IIb/IIIa receptor[1]
In Vitro

The effects of site occupancy by Sibrafiban on platelet activation are assessed using P-selectin expression, fibrinogen binding and microaggregate formation. Sibrafiban inhibits ADP and TRAP-stimulated fibrinogen binding and microaggregate formation in a concentration-dependent manner, whereas P-selectin expression is relatively unaltered. A decrease in site occupancy from peak to trough of Sibrafiban does not result in increased activation of platelets[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo

The effects of Ro 44-3888 on the platelet aggregation response to ADP (17 μmol) and on cutaneous bleeding times is determined in 8 rhesus monkeys given Sibrafiban 0.25 mg/kg/day or 0.5 mg/kg/day orally for 8 days. The maximum inhibition of ex vivo platelet aggregation and prolongation of bleeding time by Ro 44-3888 are dose dependent[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

420.46

Appearance

Solid

Formula

C20H28N4O6
CAS No.
SMILES

O=C(OCC)COC1CCN(C([[email protected]@H](NC(C2=CC=C(/C(N)=N/O)C=C2)=O)C)=O)CC1.[(Z)]
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (79.27 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3783 mL 11.8917 mL 23.7835 mL
5 mM 0.4757 mL 2.3783 mL 4.7567 mL
10 mM 0.2378 mL 1.1892 mL 2.3783 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.95 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.95 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.95 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.67%

COA (245 KB) HNMR (289 KB) LCMS (395 KB)

Handling Instructions (2659 KB)
References
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Help & FAQs
  • 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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Keywords:

Sibrafiban172927-65-0RO 48-3657IntegrinRo 44-3888orallynonpeptidedouble-prodrugglycoprotein-IIbglycoprotein-IIIaantiplateletInhibitorinhibitorinhibit

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