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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 211254-73-8
- 分子式: C28H29F5O3
- 分子量:508.52
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
IC50: 3.6 pM (progesterone receptor A), 2.5 pM (progesterone receptor B)
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CV-1 | IC50 |
54 nM
Compound: ZK-230211
|
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
|
[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] |
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
化学情報
-
CAS 番号 211254-73-8
-
分子量 508.52
-
分子式 C28H29F5O3
-
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
-
別名
ZK 230211; BAY86 5044
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)