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Merck
CN

SML4204

Yaddle1

≥98% (HPLC), powder, Piezo1 Agonist

Synonym(s):

2-{[2-Chloro-6-(trifluoromethyl)benzyl]thio}-5-(pyrazin-2-yl)-1,3,4-oxadiazole, Pyrazine, 2-[5-[[[2-chloro-6-(trifluoromethyl)phenyl]methyl]thio]-1,3,4-oxadiazol-2-yl]- (ACI)

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About This Item

Empirical Formula (Hill Notation):
C14H8ClF3N4OS
CAS Number:
Molecular Weight:
372.75
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
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Quality Level

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

General description

Yaddle1 is designed to interact specifically with the Piezo1 channel. It features a trifluoromethyl group, which is crucial for its agonistic activity.

Application

Yaddle1 may be used in immunology as a vaccine adjuvant, targeting optimal T cell activation, enhancing vaccine efficacy. It may also be used to study the role of piezo-type mechanosensitive ion channel component 1 in inflammatory bowel disease.

Biochem/physiol Actions

Yaddle1 is a mechanosensitive ion channel Piezo1 agonist with higher potency (Ca2+ influx EC50/Emax = 0.40 μM/2.6-fold using Piezo1 mCherry-expressing HEK293A) and greatly improved aqueous solubility (26.7 μM at pH 7.4) than Yoda1 (EC50/Emax = 0.50 μM/2.4-fold; solubility = 1.2 μM at pH 7.4). Yaddle1 binds to Piezo1 channel, stabilizing the open conformation of the Piezo1 channel and lowering the mechanical activation threshold.


pictograms

Exclamation mark

signalword

Warning

hcodes

Hazard Classifications

Acute Tox. 4 Oral

Storage Class

11 - Combustible Solids

flash_point_f

Not applicable

flash_point_c

Not applicable

Regulatory Information

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Sunny Goon et al.
Journal of medicinal chemistry, 67(10), 8225-8246 (2024-05-08)
Piezo1, a mechano-activated ion channel, has wide-ranging physiological and therapeutic implications, with the ongoing development of specific agonists unveiling cellular responses to mechanical stimuli. In our study, we systematically analyzed the chemical subunits in Piezo1 protein agonist Yoda1 to comprehend



Global Trade Item Number

SKUGTIN
SML4204-5MG04065273332254
SML4204-25MG04065273332247