AXT-914
Based on 1 Customer Validation
AXT-914 is a negative allosteric modulator/antagonist of the mutated calcium-sensing receptor (CaSR). AXT-914 reduces the sensitivity of the receptor to extracellular calcium, corrects the hyperresponsive state, inhibits extracellular calcium-induced intracellular calcium mobilization, and attenuates excessive cytoplasmic calcium signaling. AXT-914 can be used in the research of autosomal dominant hypocalcemia and type 5 Bartter syndrome.
For research use only. We do not sell to patients.
- Purity : 98.83%
- CAS No.: 717104-43-3
- Formula: C27H23BrN2O2
- Molecular Weight:487.39
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Storage:Powder -20°C, 3 years , 4°C, 2 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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
All Calcium Channel Isoforms
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Biological Activity
Description
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CaSR |
In Vitro
AXT-914 significantly attenuates excessive cytoplasmic calcium signaling induced by all BS type 5 and ADH-activated CaSR mutants expressed in HEK 293T cells, reducing their activity to the level of wild-type CaSR[2].
AXT-914 significantly attenuates excessive cytoplasmic calcium signaling of all BS type 5 and ADH-activated CaSR mutants co-expressed with wild-type CaSR in HEK 293T cells, reducing their activity to the level of wild-type CaSR[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 717104-43-3
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Appearance Solid
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Molecular Weight 487.39
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Formula C27H23BrN2O2
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Color Light yellow to yellow
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SMILES
O=C1N=C(C2=C(N1CC3=CC=C(C=C3)Br)C=CC(OCC#C)=C2)C4=CC=C(C(C)C)C=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (205.17 mM; Need ultrasonic; 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)
Purity & Documentation
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Data Sheet (290 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Park SY, et al. Identification and characterization of D410E, a novel mutation in the loop 3 domain of CASR, in autosomal dominant hypocalcemia and a therapeutic approach using a novel calcilytic, AXT914. Clin Endocrinol (Oxf). 2013;78(5):687-693. [Content Brief]
[2]. Letz S, et al. Amino alcohol- (NPS-2143) and quinazolinone-derived calcilytics (ATF936 and AXT914) differentially mitigate excessive signalling of calcium-sensing receptor mutants causing Bartter syndrome Type 5 and autosomal dominant hypocalcemia. PLoS One. 2014;9(12):e115178. Published 2014 Dec 15. [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 | 2.0517 mL | 10.2587 mL | 20.5174 mL | 51.2936 mL |
| 5 mM | 0.4103 mL | 2.0517 mL | 4.1035 mL | 10.2587 mL | |
| 10 mM | 0.2052 mL | 1.0259 mL | 2.0517 mL | 5.1294 mL | |
| 15 mM | 0.1368 mL | 0.6839 mL | 1.3678 mL | 3.4196 mL | |
| 20 mM | 0.1026 mL | 0.5129 mL | 1.0259 mL | 2.5647 mL | |
| 25 mM | 0.0821 mL | 0.4103 mL | 0.8207 mL | 2.0517 mL | |
| 30 mM | 0.0684 mL | 0.3420 mL | 0.6839 mL | 1.7098 mL | |
| 40 mM | 0.0513 mL | 0.2565 mL | 0.5129 mL | 1.2823 mL | |
| 50 mM | 0.0410 mL | 0.2052 mL | 0.4103 mL | 1.0259 mL | |
| 60 mM | 0.0342 mL | 0.1710 mL | 0.3420 mL | 0.8549 mL | |
| 80 mM | 0.0256 mL | 0.1282 mL | 0.2565 mL | 0.6412 mL | |
| 100 mM | 0.0205 mL | 0.1026 mL | 0.2052 mL | 0.5129 mL |
AXT-914 Related Classifications
HY-177303 Related Classifications
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Keywords
- AXT-914
- 717104-43-3
- AXT914
- AXT 914
- CaSR
- Calcium Channel
- autosomal dominant hypocalcemia
- CASR D410E
- extracellular calcium
- HEK293 cells
- cytosolic calcium signaling
- intracellular calcium mobilization
- calcium-sensing receptor
- Bartter Syndrome Type 5
- Bartter Syndrome Type 5-associated mutants
- ADH-associated mutants
- Inhibitor
- inhibitor
- inhibit