Encaleret sodium
Encaleret (CLTX-305) sodium is an orally active antagonist of the calcium-sensing receptor (CaSR), with an IC50 of 12 nM. Encaleret sodium exerts its effect by inhibiting the excessive activity of functional gain-of-function CaSR variants, and can restore blood calcium levels, promote the secretion of parathyroid hormone, improve magnesium and phosphorus metabolism, and increase urinary calcium excretion. Encaleret sodium can be used in the research of diseases such as osteoporosis and autosomal dominant hypocalcemia type 1.
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- CAS No.: 787584-62-7
- Formule: C29H32ClFNNaO4
- Masse moléculaire:536.01
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
Chemical Information
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CAS No. 787584-62-7
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Masse moléculaire 536.01
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Formule C29H32ClFNNaO4
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SMILES
FC(C=C1CC(C)(C)NC[C@@H](O)CO[C@@H](C2=C(C3=CC(C)=C(C=C3)C(O[Na])=O)C=CC=C2)C)=C(C=C1)Cl
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Synonyms
CLTX-305 sodium; JTT-305 sodium; MK-5442 sodium
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
Pureté et documentation
Références
[1]. Shinagawa Y, et al. Discovery of a potent and short-acting oral calcilytic with a pulsatile secretion of parathyroid hormone. ACS Med Chem Lett. 2010 Dec 29;2(3):238-42. [Content Brief]
[2]. Gafni RI, et al. Efficacy and Safety of Encaleret in Autosomal Dominant Hypocalcemia Type 1. N Engl J Med. 2023 Sep 28;389(13):1245-1247. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Encaleret sodium Related Classifications
HY-14401B Related Classifications
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