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PGlu-3-methyl-His-Pro-NH2 TFA (Synonyms: A-42872 TFA)

Cat. No.: HY-107380A Purity: 96.55%
Handling Instructions

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.

For research use only. We do not sell to patients.

PGlu-3-methyl-His-Pro-NH2 TFA Chemical Structure

PGlu-3-methyl-His-Pro-NH2 TFA Chemical Structure

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 238 In-stock
Estimated Time of Arrival: December 31
5 mg USD 220 In-stock
Estimated Time of Arrival: December 31
10 mg USD 360 In-stock
Estimated Time of Arrival: December 31
25 mg USD 720 In-stock
Estimated Time of Arrival: December 31
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Description

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].

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].

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.
Molecular Weight

490.43

Formula

C₁₉H₂₅F₃N₆O₆

SMILES

CN1C(C[[email protected]](NC([[email protected]@H](N2)CCC2=O)=O)C(N3[[email protected]@H](CCC3)C(N)=O)=O)=CN=C1.OC(C(F)(F)F)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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Keywords:

PGlu-3-methyl-His-Pro-NH2A-42872A42872A 42872OthersanaloguesTRHreceptorTSHpermeabilityenhancerspenetrationInhibitorinhibitorinhibit

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PGlu-3-methyl-His-Pro-NH2 TFA
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HY-107380A
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