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 changes the effects of FSH at the receptor level. FSH receptor-binding inhibitor fragment(bi-10) causes ovulation suppression and follicular atresia in mice. FSH receptor-binding inhibitor fragment (bi-10) inhibits ovarian cancer by down-regulating the overexpression of FSHR and ERβ in the ovary.

Physicochemical Properties

Molecular Formula	C42H67N13O19
Molecular Weight	1058.06
Exact Mass	1057.467
CAS #	163973-98-6
PubChem CID	131849328
Appearance	White to off-white solid powder
Density	1.4±0.1 g/cm3
Boiling Point	1757.1±65.0 °C at 760 mmHg
Flash Point	1016.4±34.3 °C
Vapour Pressure	0.0±0.6 mmHg at 25°C
Index of Refraction	1.578
LogP	-5.91
Hydrogen Bond Donor Count	16
Hydrogen Bond Acceptor Count	20
Rotatable Bond Count	34
Heavy Atom Count	74
Complexity	2120
Defined Atom Stereocenter Count	9
SMILES	C[C@H]([C@@H](C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)O)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(=O)N)C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)NCC(=O)N)N)O
InChi Key	DBFABWRXHHOYAV-JATBZIBASA-N
InChi Code	InChI=1S/C42H67N13O19/c1-18(2)13-23(52-39(71)25(15-28(44)58)53-37(69)21(7-10-32(63)64)50-41(73)34(46)19(3)56)38(70)51-22(8-11-33(65)66)42(74)55-12-4-5-26(55)40(72)54-24(14-27(43)57)36(68)48-17-30(60)49-20(6-9-31(61)62)35(67)47-16-29(45)59/h18-26,34,56H,4-17,46H2,1-3H3,(H2,43,57)(H2,44,58)(H2,45,59)(H,47,67)(H,48,68)(H,49,60)(H,50,73)(H,51,70)(H,52,71)(H,53,69)(H,54,72)(H,61,62)(H,63,64)(H,65,66)/t19-,20+,21+,22+,23+,24+,25+,26+,34+/m1/s1
Chemical Name	(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
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

ln Vivo	At high doses (30 mg/kg-40 mg/kg), ovarian and follicle development can be inhibited by FSH receptor-binding inhibitor fragment (bi-10) (10, 20, 30, 40 mg/kg; intramuscular injection; once daily; for 5 consecutive days) reducing the expression levels of ERβ and FSHR mRNA and protein in the ovary and inhibiting the production of E2[1].
Animal Protocol	Animal/Disease Models: Prepuberty Kunming female mice of 21-days old and body weight of 22.3±1.52g[1] Doses: 10, 20, 30, 40 mg/kg Route of Administration: intramuscular (im) injection; one time/day for five days Experimental Results: 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.
References	[1]. 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.

Solubility Data

Solubility (In Vitro)

May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples

Solubility (In Vivo)

Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples. Injection Formulations (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] *Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Oral Formulations Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	0.9451 mL	4.7256 mL	9.4513 mL
	5 mM	0.1890 mL	0.9451 mL	1.8903 mL
	10 mM	0.0945 mL	0.4726 mL	0.9451 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.