THR-18

Approval Year

Substance Class	Protein Created by `admin` on `Wed Apr 02 11:28:04 GMT 2025` Edited by `admin` on `Wed Apr 02 11:28:04 GMT 2025`
Protein Type	PEPTIDE
Protein Sub Type
Sequence Origin	HUMAN
Sequence Type	COMPLETE
Record UNII	PYZ33YLR8A
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

(4S)-4-(((2S)-1-((2S)-2-(((2S)-2-(((2S)-2-ACETAMIDO-5-GUANIDINO-PENTANOYL)AMINO)-4-METHYLSULFANYL-, BUTANOYL)AMINO)PROPANOYL)PYRROLIDINE-2-CARBONYL)AMINO)-5-(((1S)-1-(((1S,2S)-1-(((1S,2S)-1-(((1S)-1-(((1S)-1-(((1S)-1-((2S)-2-(((1S)-1-BENZYL-2-(((1S)-1-((

Preferred Name

English

THR-18

Common Name

English

L-ARGININAMIDE, N2-ACETYL-L-ARGINYL-L-METHIONYL-L-ALANYL-L-PROLYL-L-.ALPHA.-GLUTAMYL-L-.ALPHA.-GLUTAMYL-L-ISOLEUCYL-L-ISOLEUCYL-L-METHIONYL-L-.ALPHA.-ASPARTYL-L-ARGINYL-L-PROLYL-L-PHENYLALANYL-L-LEUCYL-L-TYROSYL-L-VALYL-L-VALYL-, TRIFLUORACETATE

Systematic Name

English

Code System Code Type Description

CAS

1383452-03-6

Created by admin on Wed Apr 02 11:28:04 GMT 2025 , Edited by admin on Wed Apr 02 11:28:04 GMT 2025

PRIMARY

FDA UNII

PYZ33YLR8A

Created by admin on Wed Apr 02 11:28:04 GMT 2025 , Edited by admin on Wed Apr 02 11:28:04 GMT 2025

PRIMARY

Related Record Type Details


					65LL7CAV6B

THR-18 FREE PEPTIDE

PARENT -> SALT/SOLVATE

Amount:

Related Record Type Details


					65LL7CAV6B

THR-18 FREE PEPTIDE

ACTIVE MOIETY

Comments:

RESULTS: In the thromboembolic model, cerebral blood flow, measured before and up to 5.5 hours post-induction, revealed that tPA administration caused reperfusion of flow at 30 minutes post-infusion. Later on, an additional increase in reperfusion was seen in the tPA+THR-18 group, and not with tPA alone. In both models, the frequency of intracranial hemorrhage in the tPA-treated group was found to be significantly higher than the control, and this tPA effect was attenuated by THR-18. In the thromboembolic study, infarct size and brain edema were similar in the control and tPA-treated rats. However, the combination of tPA and THR-18 caused a statistically significant reduction in both parameters (infarct size 17.8 versus 25.0%, brain edema 5 versus 8%, tPA+THR-18 versus control, respectively). In the tMCAO mechanical model, infarct size and brain edema were both increased by tPA treatment as compared to the control group, and this increase was markedly diminished by THR-18 co-administration. Neurobehavioral assessment of the tMCAO animals performed at 72 hours post-stroke induction revealed significant improvements (P<0.05-0.01) in neuroscores in all groups of animals treated with peptide-tPA, as compared to the tPA monotherapy group. A significant (P<0.05) improvement in the neurological outcome was also seen in the THR-18 monoterapy group, as compared to the control animals, thus demonstrating a clear neuroprotective effect by the peptide on its own. DISCUSSION: The results support the use of THR-18 together with tPA in the thrombolytic therapy of stroke, in order to achieve better patency, less tPA-induced damage, and possibly a widening of tPA therapeutic time window.

Structural Modifications

Modification Type	Location Site	Location Type	Fragment Name	Fragment Approval
AMINO_ACID_SUBSTITUTION	[1_18]	C-TERMINUS	ARGININAMIDE, L-	29626ZE0WY
MOIETY			Trifluoroacetic acid	E5R8Z4G708
AMINO_ACID_SUBSTITUTION	[1_1]	N-TERMINUS	ACETYL ARGININE	TQ7DL04CAE

Name	Property Type	Amount	Referenced Substance	Defining	Parameters	References
MOL_WEIGHT:NUMBER(CALCULATED)	CHEMICAL
Molecular Formula	CHEMICAL