AC 265347

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Cat.No. 6165 - AC 265347 | C17H17NOS | CAS No. 1253901-26-6
Description: CaSR biased allosteric modulator
Chemical Name: α-(2,4-Dimethylphenyl)-α-methyl-2-benzothiazolemethanol
Purity: ≥99% (HPLC)
Datasheet
Citations
Literature

Biological Activity

CaSR biased allosteric modulator (pEC50 = 7.8-8.1). Calcimimetic. Displays ability to bias signalling towards the accumulation of PERK1/2 and IP1. Reduces parathyroid hormone (PTH) levels in rat serum without inducing the release of calcitonin. Exhibits no significant activation of human GABAB or type I PTH receptors. Orally active.

Technical Data

M. Wt 283.39
Formula C17H17NOS
Storage Store at +4°C
Purity ≥99% (HPLC)
CAS Number 1253901-26-6
PubChem ID 52943938
InChI Key IGSZVEPQZANNAB-UHFFFAOYSA-N
Smiles CC1=CC(C)=C(C(O)(C2=NC3=CC=CC=C3S2)C)C=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 28.34 100
ethanol 28.34 100

Preparing Stock Solutions

The following data is based on the product molecular weight 283.39. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 3.53 mL 17.64 mL 35.29 mL
5 mM 0.71 mL 3.53 mL 7.06 mL
10 mM 0.35 mL 1.76 mL 3.53 mL
50 mM 0.07 mL 0.35 mL 0.71 mL

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Product Datasheets

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References

References are publications that support the products' biological activity.

Cook et al (2015) Biased allosteric modulation at the CaS receptor engendered by structurally diverse calcimimetics. Br.J.Pharmacol. 172 185 PMID: 25220431

Ma et al (2011) Characterization of highly efficacious allosteric agonists of the human calcium-sensing receptor. J.Pharmacol.Exp.Ther. 337 275 PMID: 21239511

Leach et al (2016) Towards a structural understanding of allosteric drugs at the human calcium-sensing receptor. Cell.Res. 26 574 PMID: 27002221


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Keywords: AC 265347, supplier, AC265347, CaSR, biased, allosteric, modulator, calcimimetic, parathyroid, homrone, PTH, calcitonin, PERK1/2, IP1, accumulation, orally, active, Calcium-Sensing, Receptor, Calcium-Sensing, Receptor, Tocris Bioscience

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