PGlu-3-methyl-His-Pro-NH2 TFA
PRODUCTS SPECIFICATIONS
DESCRIPTION
Overview
| MDL | - |
|---|---|
| Molecular Weight | 490.43 |
| Molecular Formula | C19H25F3N6O6 |
| SMILES | - |
Summary
PGlu-3-methyl-His-Pro-NH2 TFA (A-42872 TFA), the modified thyrotropin-releasing hormone (TRH) peptide, enhances binding to pituitary TRH receptors and increases stimulation of thyroid-stimulating hormone (TSH) release from the pituitary. The in vitro permeability of PGlu-3-methyl-His-Pro-NH2 TFA through rat skin is increased in the presence of enhancers Ethanol and Cineole [1] [2] .
In Vitro
PGlu-3-methyl-His-Pro-NH2 TFA (A-42872 TFA) has a very high affinity for the TRH receptor in the CNS. PGlu-3-methyl-His-Pro-NH2 TFA is more potent in eliciting behavioral effects as well as being more potent in the release of both growth hormone and thyroid stimulating hormone [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
PGlu-3-methyl-His-Pro-NH2 TFA (A-42872 TFA) (300 μg/kg; i.v.) elicits a 80 % increase in cerebral blood flow. Even a minute dose of PGlu-3-methyl-His-Pro-NH2 TFA (625 ng kg-1) causes an increase in cerebral blood flow
[1]
.
The addition of 3% terpene in combination with 47% ethanol increases the penetration of PGlu-3-methyl-His-Pro-NH2 TFA (5 mg/ml; transdermal administration; 30 minutes)
[2]
.
Topical application of PGlu-3-methyl-His-Pro-NH2 TFA induces an increase in TSH serum concentration from 0.32 ng/ml to 22.9 ng/ml, respectively, after 30 min. The addition of Terpene and Ethanol in combination with TRH or PGlu-3-methyl-His-Pro-NH2 TFA, increases the TSH release to 43 and 48.4 ng/ml, respectively
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Male Sprague-Dawley rats (weighing 296–356 g) [2] |
| Dosage: | 5 mg/ml |
| Administration: | Transdermal administration; 30 minutes |
| Result: | Increased in TSH-response in the presence of enhancers (3% Cineole and 47% Ethanol) as compared to peptide without enhancers. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Sealed storage, away from moisture
| Powder | -80°C | 2 years |
|---|---|---|
| -20°C | 1 year |
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
H 2 O : 250 mg/mL ( 509.76 mM ; Need ultrasonic)
DMSO : 100 mg/mL ( 203.90 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.0390 mL | 10.1951 mL | 20.3903 mL |
| 5 mM | 0.4078 mL | 2.0390 mL | 4.0781 mL |
| 10 mM | 0.2039 mL | 1.0195 mL | 2.0390 mL |
-
1.
Add each solvent one by one: PBS
Solubility: 100 mg/mL (203.90 mM); Clear solution; Need ultrasonic
References
- [1] Koskinen LO, et al. Cerebrovascular effects of the TRH analogues pGlu-3-methyl-His-Pro amide and pGlu-Glu-Pro amide: a comparison with TRH. Ups J Med Sci. 2000;105(1):73-83.
- [2] Magnusson BM, et al. Biological effects after percutaneous absorption of thyrotropin-releasing hormone and its analogue M-TRH. Peptides. 2001 Jan;22(1):73-9.