CP 376395

Name: CP 376395
Brand: MedChemExpress
SKU: HY-14130
Rating: 4.5 (1 reviews)

Cat. No.: HY-14130 Purity: 99.68%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

CP 376395 is a potent, selective, and brain-penetrable Corticotropin releasing factor 1 (CRF1) receptor antagonist.

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

CP 376395 Chemical Structure

CAS No. : 175140-00-8

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 116	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 116	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 106	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 171	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 342	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 544	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 860	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of CP 376395:

CP 376395 hydrochloride Get quote

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CRFR1 CRFR2

Biological Activity
Purity & Documentation
References
Customer Review

Description

CP 376395 is a potent, selective, and brain-penetrable Corticotropin releasing factor 1 (CRF1) receptor antagonist^[1]^[2].

IC₅₀ & Target

CRFR1

CRFR2

Cellular Effect

Cell Line	Type	Value	Description	References
IMR-32	IC₅₀	5.1 nM Compound: 11, CP-376395	Displacement of [125I]-sauvagine from rat CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting Displacement of [125I]-sauvagine from rat CRF-1 receptor expressed in human IMR-32 cells after 2 hrs by scintillation counting	[PMID: 21618986]

In Vitro

CP 376395 fully antagonizes oCRF-stimulated adenylate cyclase activity in rat cerebral cortex and at human CRF1 receptors with an apparent K_i value of 12 nM, indicating antagonist functional activity. It is highly selective for the human CRF1 receptor subtype; affinity for the CRF2 receptor is >10000 nM. It shows affinities greater than 1 µM against 40 neurotransmitter receptor and ion channels^[1].

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

In Vivo

CP 376395 (10-20 mg/kg, i.p., Male B6 mice) attenuates H2O and food intake, increases sucrose intake, attenuates EtOH intake but not EtOH preference^[2].

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

Animal Model:	Male B6 mice (n=8-9 per group)^[2]
Dosage:	0.0, 10.0, or 20.0 mg/kg
Administration:	Intraperitoneally
Result:	Dose-dependently attenuated intake of H2O and food, with H2O intake affected specifically during the first half of the session.

Molecular Weight

326.48

Formula

C₂₁H₃₀N₂O

CAS No.

175140-00-8

Appearance

Solid

Color

White to off-white

SMILES

CCC(CC)NC1=C(C)C(OC2=C(C)C=C(C)C=C2C)=NC(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 : ≥ 100 mg/mL (306.30 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	3.0630 mL	15.3149 mL	30.6297 mL
5 mM	0.6126 mL	3.0630 mL	6.1259 mL
10 mM	0.3063 mL	1.5315 mL	3.0630 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

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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: ≥ 2.5 mg/mL (7.66 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: 2.5 mg/mL (7.66 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (7.66 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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: 99.68%

Select Batch:

Data Sheet (273 KB) SDS (252 KB)

COA (247 KB) LCMS (93 KB)

Handling Instructions (2659 KB)

References

[1]. Chen YL, et al. 2-aryloxy-4-alkylaminopyridines: discovery of novel corticotropin-releasing factor 1 antagonists. J Med Chem. 2008 Mar 13;51(5):1385-92. [Content Brief]

[2]. Giardino WJ, et al. CRF1 receptor signaling regulates food and fluid intake in the drinking-in-the-dark model of binge alcohol consumption. Alcohol Clin Exp Res. 2013 Jul;37(7):1161-70. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.0630 mL	15.3149 mL	30.6297 mL	76.5744 mL
	5 mM	0.6126 mL	3.0630 mL	6.1259 mL	15.3149 mL
	10 mM	0.3063 mL	1.5315 mL	3.0630 mL	7.6574 mL
	15 mM	0.2042 mL	1.0210 mL	2.0420 mL	5.1050 mL
	20 mM	0.1531 mL	0.7657 mL	1.5315 mL	3.8287 mL
	25 mM	0.1225 mL	0.6126 mL	1.2252 mL	3.0630 mL
	30 mM	0.1021 mL	0.5105 mL	1.0210 mL	2.5525 mL
	40 mM	0.0766 mL	0.3829 mL	0.7657 mL	1.9144 mL
	50 mM	0.0613 mL	0.3063 mL	0.6126 mL	1.5315 mL
	60 mM	0.0510 mL	0.2552 mL	0.5105 mL	1.2762 mL
	80 mM	0.0383 mL	0.1914 mL	0.3829 mL	0.9572 mL
	100 mM	0.0306 mL	0.1531 mL	0.3063 mL	0.7657 mL

CP 376395 Related Classifications

Neurological Disease Endocrinology

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:

CP 376395175140-00-8CP376395CP-376395CRFRCorticotropin-releasing Factor ReceptorCRHRInhibitorinhibitorinhibit

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CP 376395

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Other Forms of CP 376395:

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Complete Stock Solution Preparation Table

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