| Identification | Back Directory | [Name]
FSH RECEPTOR-BINDING INHIBITOR FRAGMENT (BI-10) | [CAS]
163973-98-6 | [Synonyms]
H-THR-GLU-ASN-LEU-GLU-PRO-ASN-GLY-GLU-GLY-NH2
FSH RECEPTOR-BINDING INHIBITOR FRAGMENT (BI-10)
Glycinamide, L-threonyl-L-α-glutamyl-L-asparaginyl-L-leucyl-L-α-glutamyl-L-prolyl-L-asparaginylglycyl-L-α-glutamyl- (9CI)
(4S)-4-[[2-[[(2S)-4-amino-2-[[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-2-[[(2S,3R)-2-amino-3-hydroxybutanoyl]amino]-4-carboxybutanoyl]amino]-4-oxobutanoyl]amino]-4-methylpentanoyl]amino]-4-carboxybutanoyl]pyrrolidine-2-carbonyl]amino]-4-oxobutanoyl]amino]acetyl]amino]-5-[(2-amino-2-oxoethyl)amino]-5-oxopentanoic acid | [Molecular Formula]
C42H67N13O19 | [MDL Number]
MFCD00677050 | [MOL File]
163973-98-6.mol | [Molecular Weight]
1058.06 |
| Chemical Properties | Back Directory | [Boiling point ]
1757.1±65.0 °C(Predicted) | [density ]
1.420±0.06 g/cm3(Predicted) | [storage temp. ]
-15°C
| [form ]
Solid | [pka]
4.41±0.10(Predicted) | [color ]
White to off-white | [Sequence]
Thr-Glu-Asn-Leu-Glu-Pro-Asn-Gly-Glu-Gly-NH2 |
| Hazard Information | Back Directory | [Uses]
FSH receptor-binding inhibitor fragment(bi-10) is a potent FSH antagonist. FSH receptor-binding inhibitor fragment(bi-10) blocks the binding of FSH to FSHR, and alteres FSH action at the receptor level. FSH receptor-binding inhibitor fragment(bi-10) results in the suppression of ovulation and causes follicular atresia of mice. FSH receptor-binding inhibitor fragment(bi-10) has the potential for utilizing to restrain the carcinogenesis of ovarian cancer by down-regulating overexpression of FSHR and ERβ in the ovaries[1]. | [in vivo]
FSH receptor-binding inhibitor fragment(bi-10) (10, 20, 30, 40 mg/kg; Intramuscularly injection; once a day for five consecutive days) with high dose (30 mg/kg to 40 mg/kg) can suppress ovarian and follicular development, and attenuate expression levels of ERβ and FSHR mRNAs and proteins in the ovaries, additionally inhibit E2 production[1]. | Animal Model: | Prepuberty Kunming female mice of 21-days old and body weight of 22.3±1.52g[1] | | Dosage: | 10, 20, 30, 40 mg/kg | | Administration: | Intramuscularly injection; once a day for five consecutive days | | Result: | Could attenuate FSH promoting effect on the follicular development, resulting in the poor maturation of ovarian follicles.
High dose (40mg/kg) treatment blocked the follicle development of mice.
High dose of FRBI (40mg/kg) treatment blocked the follicle development of mice.
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| [References]
[1] Gong Zhuandi, et al. FSH receptor binding inhibitor restrains follicular development and possibly attenuates carcinogenesis of ovarian cancer through down-regulating expression levels of FSHR and ERβ in normal ovarian tissues. Gene. 2018 Aug 20;668:174-181. DOI:10.1016/j.gene.2018.05.068 |
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