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LH-RH (7-10) 38482-71-2

LH-RH (7-10) 38482-71-2

CAS No.: 38482-71-2

LH-RH (7-10) is a tetrapeptide and one of the main degradation products of gonadotropin-releasing hormone (LHRH) degrade
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LH-RH (7-10) is a tetrapeptide and one of the main degradation products of gonadotropin-releasing hormone (LHRH) degraded by the pituitary gland and hypothalamus. LH-RH (7-10) is produced in macrophages, type I-like and type II pneumocytes.

Physicochemical Properties


Molecular Formula C19H36N8O4
Molecular Weight 440.54034
Exact Mass 440.286
CAS # 38482-71-2
PubChem CID 3082486
Appearance Typically exists as solid at room temperature
LogP 2.359
Hydrogen Bond Donor Count 6
Hydrogen Bond Acceptor Count 6
Rotatable Bond Count 12
Heavy Atom Count 31
Complexity 678
Defined Atom Stereocenter Count 3
SMILES

NC(C(NC(C(N1CCCC1C(NCC(N)=O)=O)=O)CCCNC(=N)N)=O)CC(C)C

InChi Key JQESMPDJSXFGSA-IHRRRGAJSA-N
InChi Code

InChI=1S/C19H36N8O4/c1-11(2)9-12(20)16(29)26-13(5-3-7-24-19(22)23)18(31)27-8-4-6-14(27)17(30)25-10-15(21)28/h11-14H,3-10,20H2,1-2H3,(H2,21,28)(H,25,30)(H,26,29)(H4,22,23,24)/t12-,13-,14-/m0/s1
Chemical Name

(2S)-1-[(2S)-2-[[(2S)-2-amino-4-methylpentanoyl]amino]-5-(diaminomethylideneamino)pentanoyl]-N-(2-amino-2-oxoethyl)pyrrolidine-2-carboxamide
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 Vitro Known enzyme inhibitors, such as ACE inhibitor captopril, EP24.11 inhibitor thiorphan, and EP24.15 inhibitor ethylenediaminetetraacetic acid, reduce the production of LHRH 4-10, LHRH 7-10, and LHRH 6-10 Co-incubation[3]. With an IC50 value of 1.7 nM, LH-RH (7-10) inhibits the binding of 125I-labeled GnRH to monoclonal antibody P81662[4].
ln Vivo Esterase activity in the plasma kinin system is increased in rats by LH-RH (7-10) (iv)[1]. In the jugular vein, LH-RH (7–10) (ntracarotid infusion IV; single dosage) significantly increases the concentration of plasma LH[2].
Animal Protocol Animal/Disease Models: New Zealand White Rabbit[2]
Doses: 100, 500 and 2500 ng dissolved in 0-9% (w/v) NaCl solution and diluted
Route of Administration: Ntracarotid infusion; infused with a constant volume of 7-5 mL per 30 min
Experimental Results: Caused LH release in the female rabbit during various reproductive conditions.
References

[1]. Effect of luteinizing hormone releasing hormone fragments on the rat plasma kinin system. Russian. 1979; 69(2):115-118.

[2]. The effect of LH-RH administration on LH release in the female rabbit. J Reprod Fertil. 1979 May;56(1):175-80.

[3]. Enzymatic degradation of luteinizing hormone releasing hormone (LHRH)/[D-Ala6]-LHRH in lung pneumocytes. Pharm Res. 1998 Sep;15(9):1480-4.

[4]. Bioeffective monoclonal antibody against the decapeptide gonadotropin-releasing hormone: reacting determinant and action on ovulation and estrus suppression. Proc Natl Acad Sci U S A. 1985 Feb;82(4):1228-31.


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 2.2699 mL 11.3497 mL 22.6994 mL
5 mM 0.4540 mL 2.2699 mL 4.5399 mL
10 mM 0.2270 mL 1.1350 mL 2.2699 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.