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Cat. No.: HY-14401

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Encaleret

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

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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.

Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.

Pureté: 99.88%
CAS No.: 787583-71-5
Formule: C₂₉H₃₃ClFNO₄
Masse moléculaire:514.03

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Encaleret Chemical Structure

CAS No.: 787583-71-5

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- Cellular Effect
- In Vivo
- Essai clinique
Chemical Information
Solvant et solubilité
- In Vitro
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

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)	T_max (h)	C_max (ng/mL)	T_1/2 (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.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 787583-71-5
Appearance Solid
Masse moléculaire 514.03
Formule C₂₉H₃₃ClFNO₄
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
Synonyms

CLTX-305; JTT-305; MK-5442
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvant et solubilité

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9454 mL

9.7271 mL

19.4541 mL

5 mM

0.3891 mL

1.9454 mL

3.8908 mL

10 mM

0.1945 mL

0.9727 mL

1.9454 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (272 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

MOQ

Minimum order quantity

100 mg

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Activité biologique
- Description
- In Vivo
- Essai clinique
Chemical Information
Solvant et solubilité
- In Vitro
Pureté et documentation
Références

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Encaleret

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Orally Active Compound Library

Nuclear Receptor Compound Library

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Membrane Protein-targeted Compound Library

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Multi-Target Compound Library

Bioactive Compound Library Max

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Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Encaleret

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Clinical Compound Library

Drug Repurposing Compound Library

Orally Active Compound Library

Nuclear Receptor Compound Library

Osteogenesis Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Activité biologique

Chemical Information

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Encaleret Related Classifications

HY-14401 Related Classifications