![]() ZK168281 structure
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Common Name | ZK168281 | ||
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CAS Number | 186371-96-0 | Molecular Weight | 510.70500 | |
Density | 1.151g/cm3 | Boiling Point | 652.937ºC at 760 mmHg | |
Molecular Formula | C32H46O5 | Melting Point | N/A | |
MSDS | N/A | Flash Point | 204.377ºC |
Use of ZK168281ZK168281 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]. |
Name | Ethyl (2E)-3-{1-[(1S,3R,5Z,7E,22E,24R)-1,3,24-trihydroxy-9,10-sec ochola-5,7,10,22-tetraen-24-yl]cyclopropyl}acrylate |
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Description | 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]. |
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Related Catalog | |
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]. |
References |
Density | 1.151g/cm3 |
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Boiling Point | 652.937ºC at 760 mmHg |
Molecular Formula | C32H46O5 |
Molecular Weight | 510.70500 |
Flash Point | 204.377ºC |
Exact Mass | 510.33500 |
PSA | 86.99000 |
LogP | 5.58010 |
Vapour Pressure | 0mmHg at 25°C |
Index of Refraction | 1.578 |