Cligosiban (Synonyms: PF-3274167)

Name: Cligosiban
Brand: MedChemExpress
SKU: HY-15023
Rating: 5.0 (5 reviews)

Cat. No.: HY-15023 Purity: 99.75%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Cligosiban (PF-3274167), a high oral bioavailability and good brain-penetrant non-peptide oxytocin receptor antagonist, shows a high-affinity (K_i=9.5 nM) and an excellent selectivity versus the vasopressin receptors with almost no affinity for the V_1b and V_1a subtypes. Cligosiban inhibits ejaculatory physiology in rodents.

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

Cligosiban Chemical Structure

CAS No. : 900510-03-4

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 66	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 66	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 95	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 195	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 310	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 500	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 5 publication(s) in Google Scholar

5 Publications Citing Use of MCE Cligosiban

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•Related Screening Libraries:

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

Ki: 9.5 nM (oxytocin receptor)^[2]

Molecular Weight

419.84

Formula

C₁₉H₁₉ClFN₅O₃

CAS No.

900510-03-4

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
10 mM	0.2382 mL	1.1909 mL	2.3819 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 3 mg/mL (7.15 mM); Clear solution

This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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: 99.75%

Select Batch:

Data Sheet (277 KB) SDS (0 KB)

COA (253 KB) LCMS (88 KB)

Handling Instructions (2659 KB)

References

[1]. Wayman C, et al. Cligosiban, A Novel Brain-Penetrant, Selective Oxytocin Receptor Antagonist, Inhibits Ejaculatory Physiology in Rodents. J Sex Med. 2018 Dec;15(12):1698-1706. [Content Brief]

[2]. Karpenko IA, et al. Selective nonpeptidic fluorescent ligands for oxytocin receptor: design, synthesis, and application to time-resolved FRET binding assay. J Med Chem. 2015 Mar 12;58(5):2547-52. [Content Brief]

Complete Stock Solution Preparation Table

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

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 ReceptorOXTRInhibitorinhibitorinhibit

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Cligosiban (Synonyms: PF-3274167)

Customer Review

Cligosiban Related Antibodies

5 Publications Citing Use of MCE Cligosiban

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Purity & Documentation

References

Customer Review

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Cligosiban Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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