ZK168281
CAS No. : 186371-96-0
| Size | Price | Stock |
|---|---|---|
| 1mg | $950 | In-stock |
| 5mg | $1950 | In-stock |
| 10mg | $3200 | In-stock |
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| 100 mg | Get quote | |
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| Cat. No. : | HY-12407 |
| M.Wt: | 510.70 |
| Formula: | C32H46O5 |
| Purity: | >98 % |
| Solubility: | DMSO : 100 mg/mL (195.81 mM; Need ultrasonic) |
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[1]. IC50 & Target: Kd: 0.1 nM (VDR)[1] In Vitro: ZK168281 resembles more the mouse constitutive androstane receptor (CAR) inverse agonist Androstanol in its ability to recruit corepressor (CoR) proteins. A salt bridge between the CoR and a conserved lysine in helix 4 of the nuclear receptor (NR) is central to this interaction, but also helix 12 was stabilized by direct contacts with residues of the CoR. Fixation of helix 12 in the antagonistic/inverse agonistic conformation prevents an energetically unfavorable free floatation of the C terminus[1].
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