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ZK168281 

Cat. No. M28964
ZK168281  Structure
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Quality Control & Documentation
Biological Activity

ZK168281 is a 25-carboxylic ester 1α,25(OH)2D3 analog and a pure VDR antagonist with a Kd value of 0.1 nM. ZK168281 is an effective inhibitor of the coactivator (CoA) interaction of its receptor.

Chemical Information
Molecular Weight 510.7
Formula C32H46O5
CAS Number 186371-96-0
Form Solid
Solubility (25°C) DMSO 100 mg/mL (ultrasonic)
Storage 4°C, protect from light, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Luorui Shang, et al. Front Pharmacol. Emodin Protects Sepsis Associated Damage to the Intestinal Mucosal Barrier Through the VDR/ Nrf2 /HO-1 Pathway

[2] Daniela Rovito, et al. Nat Commun. Cytosolic sequestration of the vitamin D receptor as a therapeutic option for vitamin D-induced hypercalcemia

[3] Anna Y Belorusova, et al. J Med Chem. Structural Analysis of VDR Complex with ZK168281 Antagonist

[4] Harri Lempiäinen, et al. Mol Endocrinol. Antagonist- and inverse agonist-driven interactions of the vitamin D receptor and the constitutive androstane receptor with corepressor protein

[5] M Herdick, et al. Chem Biol. Carboxylic ester antagonists of 1alpha,25-dihydroxyvitamin D(3) show cell-specific actions

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Keywords: ZK168281  supplier, Vitamin, inhibitors, activators


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