| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
| ln Vitro |
Through the cAMP/PKA signaling inhibitor, antalarmin blocks the action of hormone-releasing factor (CRF) on Aβ1-42 levels [2].
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|---|---|
| ln Vivo |
Antalarmin (10 mg/kg; ip; daily for 4 weeks) can reduce the changes in mice's induction of chronic silent silence (CMS) [1]. Antalarmin (20 mg/kg; intraperitoneal; daily for 7 days) dramatically lowers
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| Cell Assay |
Western Blot Analysis[2]
Cell Types: Primary hippocampal neurons derived from Tg2576 mice Tested Concentrations: 100 nM Incubation Duration: 48 hrs (hours) Experimental Results: Blocked CRF-induced increase in PKAIIβ levels. |
| Animal Protocol |
Animal/Disease Models: BALB/cByJIco male mice, chronic mild stress model [1]
Doses: 10 mg/kg Route of Administration: intraperitoneal (ip) injection, every one time/day for 4 weeks. Experimental Results: Aβ1-42 levels in Tg2576 mice induced subacute anxiety [2]. The physical status of the mice was Dramatically improved. Resulting in non-significant reductions in light box (TLB) and activity compared to controls. |
| References |
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| Additional Infomation |
Antalamine is a pyrrolopyrimidine compound, chemically named 7H-pyrrolo[2,3-d]pyrimidine-4-amine, with methyl groups at positions 2, 5, and 6, a trimethylol group at position 7, and an amino group at position 4 substituted with ethyl and butyl groups. It is an antagonist of the corticotropin-releasing factor 1 (CRF-1) receptor (Ki = 1 nM). It is a pyrrolopyrimidine compound and also a tertiary amine compound.
|
| Molecular Formula |
C24H34N4
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|---|---|
| Molecular Weight |
378.55356
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| Exact Mass |
378.278
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| Elemental Analysis |
C, 76.15; H, 9.05; N, 14.80
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| CAS # |
157284-96-3
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| Related CAS # |
Antalarmin hydrochloride;220953-69-5
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| PubChem CID |
177990
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| Appearance |
Light yellow to green yellow solid powder
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| Density |
1.05g/cm3
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| Boiling Point |
437.2ºC at 760mmHg
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| Flash Point |
218.2ºC
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| Vapour Pressure |
7.63E-08mmHg at 25°C
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| Index of Refraction |
1.574
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| LogP |
5.897
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
28
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| Complexity |
485
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
CCN(C1=NC(C)=NC2N(C(=C(C)C1=2)C)C1C(C)=CC(C)=CC=1C)C(C)(C)C
|
| InChi Key |
IXPROWGEHNVJOY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H34N4/c1-9-11-12-27(10-2)23-21-18(6)19(7)28(24(21)26-20(8)25-23)22-16(4)13-15(3)14-17(22)5/h13-14H,9-12H2,1-8H3
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| Chemical Name |
N-butyl-N-ethyl-2,5,6-trimethyl-7-(2,4,6-trimethylphenyl)pyrrolo[2,3-d]pyrimidin-4-amine
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| Synonyms |
Antalarmin
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| HS Tariff Code |
2934.99.03.00
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO: ~20.8 mg/mL (~55.0 mM; with ultrasonication and warming by heating to 60°C)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.60 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), Clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (6.60 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Suspended solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (6.60 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.2642 mL | 1.3208 mL | 2.6417 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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