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

Antalarmin is a selective nonpeptide corticotropin-releasing factor receptor 1 (CRHR1) antagonist with a Ki of 2.7 nM. Antalarmin can pass through the blood–brain barrier.

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

Antalarmin Chemical Structure

Antalarmin Chemical Structure

CAS No. : 157284-96-3

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10 mg USD 490 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Antalarmin:

Antalarmin Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Antalarmin

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Antalarmin is a selective nonpeptide corticotropin-releasing factor receptor 1 (CRHR1) antagonist with a Ki of 2.7 nM. Antalarmin can pass through the blood–brain barrier[1][2][3].

IC50 & Target

Ki: 2.7 nM (CRHR1)[3]
In Vitro

Antalarmin inhibits the effect of corticotrophin-releasing factor (CRF) on Aβ1-42 levels through the cAMP/PKA signaling pathway[2].

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

Antalarmin Related Antibodies

Western Blot Analysis[2]

Cell Line: Primary hippocampal neurons derived from Tg2576 mice
Concentration: 100 nM
Incubation Time: 48 h
Result: Blocked CRF-induced increases in PKAIIβ levels.
In Vivo

Antalarmin (10 mg/kg; i.p.; daily for 4 weeks) leads to an improvement of chronic mild stress (CMS)-induced modifications in mice[1].
Antalarmin (20 mg/kg; i.p.; daily for 7 days) significantly reduces Aβ1-42 levels in sub-acute stressed Tg2576 mice[2].

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

Animal Model: BALB/cByJIco male mice, chronic mild stress model[1]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection, daily for 4 weeks
Result: Induced a significant improvement of mice physical state. Induced a nonsignificant decrease of the lit box (TLB) and activity when compared to controls.
Molecular Weight

378.55

Formula

C24H34N4
CAS No.
Appearance

Solid

SMILES

CC1=C(N2C(C)=C(C)C3=C(N(CCCC)CC)N=C(C)N=C32)C(C)=CC(C)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (66.04 mM; ultrasonic and warming and heat to 60°C; 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 2.6417 mL 13.2083 mL 26.4166 mL
5 mM 0.5283 mL 2.6417 mL 5.2833 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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. 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 1 mM 2.6417 mL 13.2083 mL 26.4166 mL 66.0415 mL
5 mM 0.5283 mL 2.6417 mL 5.2833 mL 13.2083 mL
10 mM 0.2642 mL 1.3208 mL 2.6417 mL 6.6041 mL
15 mM 0.1761 mL 0.8806 mL 1.7611 mL 4.4028 mL
20 mM 0.1321 mL 0.6604 mL 1.3208 mL 3.3021 mL
25 mM 0.1057 mL 0.5283 mL 1.0567 mL 2.6417 mL
30 mM 0.0881 mL 0.4403 mL 0.8806 mL 2.2014 mL
40 mM 0.0660 mL 0.3302 mL 0.6604 mL 1.6510 mL
50 mM 0.0528 mL 0.2642 mL 0.5283 mL 1.3208 mL
60 mM 0.0440 mL 0.2201 mL 0.4403 mL 1.1007 mL
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Antalarmin 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:

Antalarmin157284-96-3CRFRCorticotropin-releasing Factor ReceptorCRHRblood–brain barrierBBBCRHR1corticotropin-releasing factor receptorcorticotrophin-releasing factorCRFAβ1-42Inhibitorinhibitorinhibit

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