Encaleret
CAS No. : 787583-71-5
(Synonyms: CLTX-305; JTT-305; MK-5442)
| Size | Price | Stock |
|---|---|---|
| 5mg | $400 | In-stock |
| 10mg | $650 | In-stock |
| 25mg | $1340 | In-stock |
| 50mg | $2150 | In-stock |
| 100mg | $3480 | In-stock |
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| Cat. No. : | HY-14401 |
| M.Wt: | 514.03 |
| Formula: | C29H33ClFNO4 |
| Purity: | >98 % |
| Solubility: | DMSO : 350 mg/mL (ultrasonic) |
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].
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 |