Antalarmin
Based on 7 publication(s) in Google Scholar
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.
- Purity: 99.95%
- CAS No.: 157284-96-3
- Formula: C24H34N4
- Molecular Weight:378.55
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Antalarmin
More- Immunity. 2026 Mar 10;59(3):598-617.e11. [Abstract]
- Immunity. 2024 Feb 13;57(2):364-378.e9. [Abstract]
- Sci Adv. 2026 May 15;12(20):eaeb6961. [Abstract]
- J Agric Food Chem. 2026 Jan 28;74(3):2560-2573. [Abstract]
- Ann Med. 2025 Dec;57(1):2490823. [Abstract]
- Exp Neurol. 2024 May 30:114822. [Abstract]
- SSRN. 2025 Jun 18.
Biological Activity
Ki: 2.7 nM (CRHR1)[3]
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.
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Cell Line:Primary hippocampal neurons derived from Tg2576 mice
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Concentration:100 nM
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Incubation Time:48 h
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Result:Blocked CRF-induced increases in PKAIIβ levels.
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.
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Animal Model:BALB/cByJIco male mice, chronic mild stress model[1]
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Dosage:10 mg/kg
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Administration:Intraperitoneal injection, daily for 4 weeks
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Result:Induced a significant improvement of mice physical state. Induced a nonsignificant decrease of the lit box (TLB) and activity when compared to controls.
Chemical Information
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CAS No. 157284-96-3
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Appearance Solid
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Molecular Weight 378.55
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Formula C24H34N4
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Color White to light yellow
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SMILES
CC1=C(N2C(C)=C(C)C3=C(N(CCCC)CC)N=C(C)N=C32)C(C)=CC(C)=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (7)
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Journal Impact Factor
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Most Recent
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Immunity
2026 Mar 10;59(3):598-617.e11. PMID: 41722568 -
Immunity
Small-molecule CBP/p300 histone acetyltransferase inhibition mobilizes leukocytes from the bone marrow via the endocrine stress response. [Abstract]2024 Feb 13;57(2):364-378.e9. PMID: 38301651 -
Sci Adv
2026 May 15;12(20):eaeb6961. PMID: 42139357 -
J Agric Food Chem
Peoniflorin Alleviates Corticotropin-Releasing Factor-Induced Irritable Bowel Syndrome by Improving the Intestinal Barrier Function through the Inhibition of the CRFR1/ROCK2/MLC Signaling Pathway. [Abstract]2026 Jan 28;74(3):2560-2573. PMID: 41550014 -
Ann Med
Corticotropin-releasing hormone inhibits autophagy by suppressing PTEN to promote apoptosis in dermal papilla cells. [Abstract]2025 Dec;57(1):2490823. PMID: 40219757 -
Exp Neurol
CRHR1 antagonist alleviated depression-like behavior by downregulating p62 in a rat model of post-stroke depression. [Abstract]2024 May 30:114822. PMID: 38823676 -
Solvent & Solubility
DMSO : 20.83 mg/mL (55.03 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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.60 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (6.60 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (279 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Ducottet C, et al. Effects of the selective nonpeptide corticotropin-releasing factor receptor 1 antagonist antalarmin in the chronic mild stress model of depression in mice. Prog Neuropsychopharmacol Biol Psychiatry. 2003 Jun;27(4):625-31. [Content Brief]
[2]. Dong H, et al. Effects of corticotrophin-releasing factor receptor 1 antagonists on amyloid-β and behavior in Tg2576 mice. Psychopharmacology (Berl). 2014 Dec;231(24):4711-22. [Content Brief]
[3]. Zorrilla EP, et al. Urocortin shares the memory modulating effects of corticotropin-releasing factor (CRF): mediation by CRF1 receptors. Brain Res. 2002 Oct 18;952(2):200-10. [Content Brief]
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 |
Antalarmin Related Classifications
HY-124475 Related Classifications
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