2. GPCR/G Protein
  3. CRFR
  4. Antalarmin hydrochloride

Antalarmin (hydrochloride) is an oral active non-peptide corticotropin-releasing hormone receptor 1 (CRHR1) antagonist with a Ki of 1 nM. Antalarmin hydrochloride suppresses CRH-induced ACTH secretion and blocks CRH and novelty induced anxiety-like behavior in animal models. Antalarmin hydrochloride produces anti-inflammatory effects in arthritis models, and suppresses stress-induced gastric ulceration related to irritable bowel syndrome.

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Antalarmin hydrochloride Chemical Structure

Antalarmin hydrochloride Chemical Structure

CAS No. : 220953-69-5

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Based on 2 publication(s) in Google Scholar

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Antalarmin hydrochloride Related Antibodies

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Description

Antalarmin (hydrochloride) is an oral active non-peptide corticotropin-releasing hormone receptor 1 (CRHR1) antagonist with a Ki of 1 nM. Antalarmin hydrochloride suppresses CRH-induced ACTH secretion and blocks CRH and novelty induced anxiety-like behavior in animal models. Antalarmin hydrochloride produces anti-inflammatory effects in arthritis models, and suppresses stress-induced gastric ulceration related to irritable bowel syndrome[1][2][3].

In Vitro

Antalarmin (1 µM, 10 minutes) blocks CRH-induced cAMP increase and VEGF production in human mast cells (HMC-1 and hCBMC cells) via CRH-R1[4].

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

Antalarmin hydrochloride Related Antibodies
In Vivo

Antalarmin hydrochloride (5, 10, 20 mg/kg, i.p., single dose) blocks CRF-induced anxiety-like behavior and reduces defensive withdrawal in rats[2].

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

Animal Model: CRF-induced anxiety-like behavior in Wistar rats (250-300 g, male)[2]
Dosage: 5, 10, 20 mg/kg
Administration: Intraperitoneal (i.p.), 80 minutes before behavioral tests, single dose
Result: Reduced defensive withdrawal behavior, blocked CRF-induced anxiety-like effects, without affecting normal behavior.
Animal Model: D-amphetamine-induced motor activation in Wistar rats[2]
Dosage: 20 mg/kg
Administration: Intraperitoneal (i.p.), 90 minutes before behavioral tests, single dose
Result: Did not affect D-amphetamine-induced motor activation.
Molecular Weight

415.01

Formula

C24H35ClN4
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

CC1=C(N2C(C)=C(C)C3=C(N(CCCC)CC)N=C(C)N=C32)C(C)=CC(C)=C1.[H]Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMF : 20 mg/mL (48.19 mM; Need ultrasonic and warming)

Ethanol : 14 mg/mL (33.73 mM; Need ultrasonic and warming)

DMSO : 12.5 mg/mL (30.12 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4096 mL 12.0479 mL 24.0958 mL
5 mM 0.4819 mL 2.4096 mL 4.8192 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  15% Cremophor EL    85% Saline

    Solubility: 5 mg/mL (12.05 mM); Clear solution; Need ultrasonic

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.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.87%

COA (253 KB) HNMR (275 KB) RP-HPLC (244 KB) LCMS (259 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / Ethanol / DMF 1 mM 2.4096 mL 12.0479 mL 24.0958 mL 60.2395 mL
5 mM 0.4819 mL 2.4096 mL 4.8192 mL 12.0479 mL
10 mM 0.2410 mL 1.2048 mL 2.4096 mL 6.0240 mL
15 mM 0.1606 mL 0.8032 mL 1.6064 mL 4.0160 mL
20 mM 0.1205 mL 0.6024 mL 1.2048 mL 3.0120 mL
25 mM 0.0964 mL 0.4819 mL 0.9638 mL 2.4096 mL
30 mM 0.0803 mL 0.4016 mL 0.8032 mL 2.0080 mL
DMF 40 mM 0.0602 mL 0.3012 mL 0.6024 mL 1.5060 mL
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Antalarmin hydrochloride 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:

Antalarmin220953-69-5CRFRCorticotropin-releasing Factor ReceptorCRHRHMC-1 and hCBMC cellsCRF-induced anxiety-like behavior modelInhibitorinhibitorinhibit

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