2. GPCR/G Protein Vitamin D Related/Nuclear Receptor
  3. CaSR Thyroid Hormone Receptor
  4. Encaleret

Encaleret  (Synonyms: CLTX-305; JTT-305; MK-5442)

Cat. No.: HY-14401 Pureza: 99.88%
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Instrucciones de manejo Technical Support

Encaleret (CLTX-305) is an orally active antagonist of the calcium-sensing receptor (CaSR), with an IC50 of 12 nM. Encaleret 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 can be used in the research of diseases such as osteoporosis and autosomal dominant hypocalcemia type 1.

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Encaleret

Encaleret Estructura química

No. CAS : 787583-71-5

Tamaño Precio Stock Cantidad
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 En stock
Solution
10 mM * 1 mL in DMSO En stock
Solid
5 mg En stock
10 mg En stock
25 mg En stock
50 mg En stock
100 mg En stock
200 mg   Obtener un presupuesto  
500 mg   Obtener un presupuesto  

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Other Forms of Encaleret:

Encaleret Related Antibodies

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Descripciòn

Encaleret (CLTX-305) is an orally active antagonist of the calcium-sensing receptor (CaSR), with an IC50 of 12 nM. Encaleret 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 can be used in the research of diseases such as osteoporosis and autosomal dominant hypocalcemia type 1[1][2].

Cellular Effect
Cell Line Type Value Description References
PC-12 IC50
0.012 μM
Compound: 15, JTT-305
Antagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assay
Antagonist activity at human CaSR expressed in rat PC12h cells by reporter gene assay
[PMID: 24900301]
In Vivo

Encaleret (1-3 mg/kg; oral administration; single dose) rapidly and transiently increases the level of endogenous parathyroid hormone in a dose-dependent manner in rats[1].
Pharmacokinetic Analysis in Rats[1]

Route Dose (mg/kg) Tmax (h) Cmax (ng/mL) T1/2 (h) BA (%)
p.o. 1 0.5 475 1.8 64

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

514.03

Fòrmula

C29H33ClFNO4
No. CAS
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=C(C2=CC=CC=C2[C@H](OC[C@H](O)CNC(C)(C)CC3=CC=C(Cl)C(F)=C3)C)C=C1C)O
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvente y solubilidad
In Vitro: 

DMSO : 175 mg/mL (340.45 mM; Need ultrasonic; 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 1.9454 mL 9.7271 mL 19.4541 mL
5 mM 0.3891 mL 1.9454 mL 3.8908 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.

  • Calculadora de molaridad

  • Calculadora de dilución

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Pureza y Documentación
Referencias

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 1.9454 mL 9.7271 mL 19.4541 mL 48.6353 mL
5 mM 0.3891 mL 1.9454 mL 3.8908 mL 9.7271 mL
10 mM 0.1945 mL 0.9727 mL 1.9454 mL 4.8635 mL
15 mM 0.1297 mL 0.6485 mL 1.2969 mL 3.2424 mL
20 mM 0.0973 mL 0.4864 mL 0.9727 mL 2.4318 mL
25 mM 0.0778 mL 0.3891 mL 0.7782 mL 1.9454 mL
30 mM 0.0648 mL 0.3242 mL 0.6485 mL 1.6212 mL
40 mM 0.0486 mL 0.2432 mL 0.4864 mL 1.2159 mL
50 mM 0.0389 mL 0.1945 mL 0.3891 mL 0.9727 mL
60 mM 0.0324 mL 0.1621 mL 0.3242 mL 0.8106 mL
80 mM 0.0243 mL 0.1216 mL 0.2432 mL 0.6079 mL
100 mM 0.0195 mL 0.0973 mL 0.1945 mL 0.4864 mL
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Encaleret 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:

Encaleret787583-71-5CLTX-305 JTT-305 MK-5442CLTX305CLTX 305JTT305JTT 305JTT-305MK5442MK 5442MK-5442CaSRThyroid Hormone ReceptorCalcium-sensing receptor THROralparathyroid hormoneInhibitorinhibitorinhibit

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Nombre del producto:
Encaleret
Cat. No.:
HY-14401
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