[D-Phe2,6, Pro3]-LH-RH
[D-Phe2,6, Pro3]-LH-RH is a potent luteinizing hormone releasing hormone (LHRH) antagonist.
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- CAS No.: 64789-67-9
- Formule: C59H80N14O13
- Masse moléculaire:1193.35
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
![[D-Phe2,6, Pro3]-LH-RH Chemical Structure](https://file.medchemexpress.com/product_pic/hy-p3666.gif "Click to View [D-Phe2,6, Pro3]-LH-RH Chemical Structure")
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
In Vitro
[D-Phe2,6, Pro3]-LH-RH (0.1 pM-1 mM; 24 h) does not alter GnRH binding capacity in pituitary cells but blocks the increase in sites induced by GnRH[2].
[D-Phe2,6, Pro3]-LH-RH (2.7 μM) causes significant increases in thyrotropin (TSH) secretion in pituitaries[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
[D-Phe2,6, Pro3]-LH-RH (750 μg, single injection at 12:00 h on the day of proestrus) inhibits ovulation in 100% of treated rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult rhesus monkeys[1]
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Dosage:300 mg/monkey
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Administration:SC, every 8 h at a dose of 50 mg/injection; six injections
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Result:Showed antagonistic activity: 1) an immediate cessation of the LU and FSH surges; 2) prolonged surges and/or abnormal, discontinuous gonadotropin secretion; 3) LH and FSH peaks of diminished magnitude; 4) the absence of concomitant LH and FSH midcycle peaks; 3) LH and FSH peaks of diminished magnitude; 4) the absence of concomitant LH and FSH midcycle peaks; 5) suppression of serum estradiol concentrations without concurrent reductions in serum gonadotropin values; or 6) a failure to identify corpora lutea at the time of laparoscopic visualization of the ovaries.
Chemical Information
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CAS No. 64789-67-9
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Masse moléculaire 1193.35
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Formule C59H80N14O13
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Sequence Shortening
{Glp}-{d-Phe}-PSY-{d-Phe}-LRPG-NH2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Solvant et solubilité
In Vitro
H2O
Peptide Solubility and Storage Guidelines:
1. Calculate the length of the peptide.
2. Calculate the overall charge of the entire peptide according to the following table:
| Contents | Assign value | |
|---|---|---|
| Acidic amino acid | Asp (D), Glu (E), and the C-terminal -COOH. | -1 |
| Basic amino acid | Arg (R), Lys (K), His (H), and the N-terminal -NH2 | +1 |
| Neutral amino acid | Gly (G), Ala (A), Leu (L), Ile (I), Val (V), Cys (C), Met (M), Thr (T), Ser (S), Phe (F), Tyr (Y), Trp (W), Pro (P), Asn (N), Gln (Q) | 0 |
3. Recommended solution:
| Overall charge of peptide | Details |
|---|---|
| Negative (<0) |
1. Try to dissolve the peptide in water first. 2. If water fails, add NH4OH (<50 μL). 3. If the peptide still does not dissolve, add DMSO (50-100 μL) to solubilize the peptide. |
| Positive (>0) |
1. Try to dissolve the peptide in water first. 2. If water fails, try dissolving the peptide in a 10%-30% acetic acid solution. 3. If the peptide still does not dissolve, try dissolving the peptide in a small amount of DMSO. |
| Zero (=0) |
1. Try to dissolve the peptide in organic solvent (acetonitrile, methanol, etc.) first. 2. For very hydrophobic peptides, try dissolving the peptide in a small amount of DMSO, and then dilute the solution with water to the desired concentration. |
Pureté et documentation
Références
[1]. Wilks JW, et al. Effect of [D-Phe2, Pro3, D-Phe6]-luteinizing hormone releasing hormone, an antagonist, on preovulatory gonadotropin secretion in the rhesus monkey. Biol Reprod. 1980 Aug;23(1):1-9. [Content Brief]
[2]. Loumaye E, et al. Homologous regulation of gonadotropin-releasing hormone receptors in cultured pituitary cells. Science. 1982 Feb 19;215(4535):983-5. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
[D-Phe2,6, Pro3]-LH-RH Related Classifications
HY-P3666 Related Classifications
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