| Identification | Back Directory | [Name]
(3aS*,4R*,9bR*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-3H-cyclopenta[c]quinoline | [CAS]
1161002-05-6 | [Synonyms]
H37
G-15
RMB5
AGPAT1
LUCA15
1-AGPAT1
LPAAT-alpha
G15;G-15;G 15;1161002-05-6
RNA binding motif protein 5
Compound G15 - GPR30 antagonist
Anti-AGPAT1 antibody produced in rabbit
(3aS*,4R*,9bR*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-3H-cyclopenta[c]quinoline
(3aR,4R,9bS)-4-(6-bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline
(3aS,4R,9bR)-4-(6-BroMo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline
3H-Cyclopenta[c]quinoline, 4-(6-bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-, (3aS,4R,9bR)-
(3aS,4R,9bR)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline (G-15) | [Molecular Formula]
C19H16BrNO2 | [MDL Number]
MFCD16618401 | [MOL File]
1161002-05-6.mol | [Molecular Weight]
370.24 |
| Chemical Properties | Back Directory | [Melting point ]
178-180 °C | [Boiling point ]
462.7±45.0 °C(Predicted) | [density ]
1.472±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
insoluble in H2O; insoluble in EtOH; ≥37 mg/mL in DMSO | [form ]
solid | [pka]
3.98±0.40(Predicted) | [color ]
White to off-white | [biological source]
rabbit |
| Hazard Information | Back Directory | [Description]
G protein-coupled estrogen receptor (GPER), or GPR30, specifically binds natural and man-made estrogens. It is thought to be involved in estrogen-sensitive cancers. GPER knockout mice are fertile, although they exhibit thymic atrophy, impaired glucose tolerance, and altered bone growth. G-15 is a cell-permeable non-steroidal antagonist of GPER (Ki = 20 nM). It displays low affinity cross-reactivity with the classical estrogen receptor (ER), ERα, so that at doses greater than 1 μM it is capable of mediating limited ER-dependent transcriptional activity. G-15 antagonizes the anti-depressive effects of estrogen in vivo. | [Uses]
(3aS,4R,9bR)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline is also known as “G-15”, a G-protein-coupled estrogen receptor antagonist designed for the treatment of estrogen-sensitive cancers. | [in vivo]
G15 (1.46 mg/kg; i.h.; twice a week for 14 weeks) decreases the number of tumor nodules and tumor index increased by the E2 or G1 group in urethane-induced adenocarcinoma mice[1]. | Animal Model: | Four-week-old female Kunming mice (Urethane-induced adenocarcinoma)[1] | | Dosage: | 1.46 mg/kg (combination with E2, 0.09 mg/kg and fulvestrant (Ful), 2.4 mg/kg) | | Administration: | Subcutaneous injection; twice a week for 14 weeks | | Result: | The number of tumor nodules decreased in the E2+Ful+G15 group. |
| [storage]
-20°C, protect from light | [References]
[1] dennis mk, burai r, ramesh c, et al. in vivo effects of a gpr30 antagonist. nat chem biol, 2009, 5 (6): 421-427.
[2] g-protein-coupled estrogen receptor and the gper-antagonist g-15 inhibits proliferation in endometriotic cells. fertil steril, 2013, 100 (3): 770-776.
[3] hammond r, nelson d, kline e, et al. chronic treatment with a gpr30 antagonist impairs acquisition of a spatial learning task in young female rats. horm behav, 2012, 62 (4): 367-374. |
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BOC Sciences
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16314854226 |
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www.bocsci.com |
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