A CaSR antagonist
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Encaleret

Item No. 45051

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2′-[(1R)-1-[(2R)-3-[[2-(4-chloro-3-fluorophenyl)-1,1-dimethylethyl]amino]-2-hydroxypropoxy]ethyl]-3-methyl-[1,1′-biphenyl]-4-carboxylic acid
CAS Number
787583-71-5
Synonyms
  • CLTX-305
  • JTT-305
  • MK-5442
Molecular Formula
C29H33ClFNO4
Formula Weight
514.0
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile:Water (1:1): Slightly soluble: 0.1-1 mg/mlDMSO: Sparingly Soluble: 1-10 mg/ml
SMILES
FC(C=C1CC(C)(C)NC[C@@H](O)CO[C@@H](C(C=CC=C2)=C2C3=CC(C)=C(C(O)=O)C=C3)C)=C(C=C1)Cl
InChi Code
InChI=1S/C29H33ClFNO4/c1-18-13-21(10-11-23(18)28(34)35)25-8-6-5-7-24(25)19(2)36-17-22(33)16-32-29(3,4)15-20-9-12-26(30)27(31)14-20/h5-14,19,22,32-33H,15-17H2,1-4H3,(H,34,35)/t19-,22-/m1/s1
InChi Key
UNFHDRVFEQPUEL-DENIHFKCSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $125

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    5 mg

    $375

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    10 mg

    $625

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    Product Description

    Encaleret is a calcium-sensing receptor (CaSR) antagonist (IC50 = 0.012 µM in a reporter assay using PC12h cells).1 Oral administration of encaleret (20 µg/g) increases plasma levels of parathyroid hormone, prevents renal calcification, and increases bone mineral density in a model of autosomal dominant hypocalcemia (ADH) using CaSR knock-in mice.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Shinagawa, Y., Inoue, T., Katsushima, T., et al. Discovery of a potent and short-acting oral calcilytic with a pulsatile secretion of parathyroid hormone. ACS Med. Chem. Lett. 2(3), 238-242 (2010).

    2. Dong, B., Endo, I., Ohnishi, Y., et al. Calcilytic ameliorates abnormalities of mutant calcium-sensing receptor (CaSR) knock-in mice mimicking autosomal dominant hypocalcemia (ADH). J. Bone Miner. Res. 30(11), 1980-1993 (2015).