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

Cligosiban  (Synonyms: PF-3274167)

Cat. No.: HY-15023 Purity: 99.88%
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Cligosiban (PF-3274167) is an orally active, highly selective, and centrally permeable oxytocin receptor antagonist with good pharmacokinetics in rats and can inhibit physiological ejaculation in rodents[1][2].

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
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 66 In-stock
Solution
10 mM * 1 mL in DMSO USD 66 In-stock
Solid
1 mg USD 30 In-stock
5 mg USD 60 In-stock
10 mg USD 95 In-stock
25 mg USD 195 In-stock
50 mg USD 310 In-stock
100 mg USD 500 In-stock
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Based on 6 publication(s) in Google Scholar

Cligosiban Related Antibodies

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Description

Cligosiban (PF-3274167) is an orally active, highly selective, and centrally permeable oxytocin receptor antagonist with good pharmacokinetics in rats and can inhibit physiological ejaculation in rodents[1][2].
IC50 & Target

oxytocin receptor[1]
In Vitro

Cligosiban (1 μM) has an antagonistic effect on endogenous release of oxytocin (OT) induced prostate motility in rats[3].
Cligosiban (1, 10 μM) can reduce the frequency of spontaneous bladder contractions in young and old rats[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cligosiban Related Antibodies
In Vivo

Cligosiban (0.9 mg/kg; 3 to 5 minutes after injection of Apomorphine (HY-12723); i.v.) shows CNS permeability and inhibits Apomorphine-induced ejaculation in an anesthetized rat CNS neuronal discharge model by modulating oxytocin (OT)-mediated responses in the nucleus tractus solitarius (NTS)[1].
Cligosiban (1 mg/kg; i.v. or p.o.) produces 4 metabolites in rat plasma, with demethylation and glucuronidation being the major metabolic pathways, and the pharmacokinetic profile is favorable[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Sprague Dawley rats (280-350 g), Anesthetized Rat CNS Neuronal Firing Model (Pre injection of Apomorphine (200 mg/kg, intravenous injection) into rats to regulate neuronal firing)[1].
Dosage: 0.9 mg/kg
Administration: Intravenous injection (i.v.); 3 to 5 minutes after injection of Apomorphine
Result: Reversed the reduced firing of nucleus tractus solitaries (NTS) neurons induced by Apomorphine and reduced the bulbospongiosum burst pattern and contraction amplitude associated with ejaculation.
Animal Model: Male Sprague-Dawley rats with body weight of 200-220 g[2].
Dosage: 1 mg/kg
Administration: Intravenous injection (i.v.) or oral gavage (p.o.)
Result: Was rapidly absorbed into the plasma after oral administration and reached its maximum blood concentration 1.41 hours after administration, and was quickly eliminated from the plasma after absorption.
Molecular Weight

419.84

Formula

C19H19ClFN5O3
CAS No.
Appearance

Solid

Color

Off-white to pink

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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (119.09 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.88%

COA (253 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3819 mL 11.9093 mL 23.8186 mL 59.5465 mL
5 mM 0.4764 mL 2.3819 mL 4.7637 mL 11.9093 mL
10 mM 0.2382 mL 1.1909 mL 2.3819 mL 5.9546 mL
15 mM 0.1588 mL 0.7940 mL 1.5879 mL 3.9698 mL
20 mM 0.1191 mL 0.5955 mL 1.1909 mL 2.9773 mL
25 mM 0.0953 mL 0.4764 mL 0.9527 mL 2.3819 mL
30 mM 0.0794 mL 0.3970 mL 0.7940 mL 1.9849 mL
40 mM 0.0595 mL 0.2977 mL 0.5955 mL 1.4887 mL
50 mM 0.0476 mL 0.2382 mL 0.4764 mL 1.1909 mL
60 mM 0.0397 mL 0.1985 mL 0.3970 mL 0.9924 mL
80 mM 0.0298 mL 0.1489 mL 0.2977 mL 0.7443 mL
100 mM 0.0238 mL 0.1191 mL 0.2382 mL 0.5955 mL
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Cligosiban Related Classifications

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.

Keywords:

Cligosiban900510-03-4PF-3274167PF3274167PF 3274167Oxytocin ReceptorOXTROxytocin receptorCNS permeabilityphysiological ejaculationInhibitorinhibitorinhibit

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