1. GPCR/G Protein
  2. Oxytocin Receptor
  3. Cligosiban

Cligosiban (Synonyms: PF-3274167)

Cat. No.: HY-15023 Purity: 99.85%
Handling Instructions

Cligosiban, a high oral bioavailability and good brain-penetrant non-peptide oxytocin receptor antagonist, shows a high-affinity (Ki=9.5 nM) and an excellent selectivity versus the vasopressin receptors with almost no affinity for the V1b and V1a subtypes. Cligosiban inhibits ejaculatory physiology in rodents.

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

Cligosiban Chemical Structure

Cligosiban Chemical Structure

CAS No. : 900510-03-4

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 238 In-stock
Estimated Time of Arrival: December 31
5 mg USD 216 In-stock
Estimated Time of Arrival: December 31
10 mg USD 312 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1152 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1920 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 2 publication(s) in Google Scholar

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Description

Cligosiban, a high oral bioavailability and good brain-penetrant non-peptide oxytocin receptor antagonist, shows a high-affinity (Ki=9.5 nM) and an excellent selectivity versus the vasopressin receptors with almost no affinity for the V1b and V1a subtypes. Cligosiban inhibits ejaculatory physiology in rodents[1][2].

IC50 & Target

Ki: 9.5 nM (oxytocin receptor)[2]

Molecular Weight

419.84

Formula

C₁₉H₁₉ClFN₅O₃

CAS No.

900510-03-4

SMILES

FC1=CC(Cl)=C(OC2CN(C3=NN=C(COC)N3C4=CC=C(OC)N=C4)C2)C=C1

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 : ≥ 50 mg/mL (119.09 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3819 mL 11.9093 mL 23.8186 mL
5 mM 0.4764 mL 2.3819 mL 4.7637 mL
10 mM 0.2382 mL 1.1909 mL 2.3819 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: ≥ 3 mg/mL (7.15 mM); Clear solution

  • 2.

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

    Solubility: ≥ 3 mg/mL (7.15 mM); Clear solution

  • 3.

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

    Solubility: ≥ 3 mg/mL (7.15 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.85%

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Cligosiban
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HY-15023
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