Lonaprisan
Lonaprisan (ZK 230211; BAY86 5044) is an antagonist for progesterone receptor, with IC50 of 3.6 pM and 2.5 pM for PR-A and PR-B, respectively. Lonaprisan exhibits antiprogestagenic activity in rabbits, interrupts early pregnancy in rats, and exhibits antitumor efficacy against DMBA (HY-W011845)-induced mammary tumor. Lonaprisan reveals antiglucocorticoid and antiandrogenic effect.
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- CAS No.: 211254-73-8
- 화학식: C28H29F5O3
- 분자량:508.52
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
IC50: 3.6 pM (progesterone receptor A), 2.5 pM (progesterone receptor B)
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CV-1 | IC50 |
54 nM
Compound: ZK-230211
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In vitro antagonist potency in transactivation assay in CV-1 cells expressing androgen receptor
In vitro antagonist potency in transactivation assay in CV-1 cells expressing androgen receptor
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[PMID: 11150172] |
| NIH3T3 | IC50 |
16 nM
Compound: ZK-230211
|
In vitro antagonist potency in transactivation assay in NIH3T3 cells expressing glucocorticoid receptor
In vitro antagonist potency in transactivation assay in NIH3T3 cells expressing glucocorticoid receptor
|
[PMID: 11150172] |
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 211254-73-8
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분자량 508.52
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화학식 C28H29F5O3
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SMILES
O=C1CCC2=C3[C@@H](C4=CC=C(C(C)=O)C=C4)C[C@@]5(C)[C@](CC[C@@]5(O)C(F)(C(F)(F)F)F)([H])[C@]3([H])CCC2=C1
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Synonyms
ZK 230211; BAY86 5044
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)