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Merck
CN

SML3396

UCSF678 HYDROCHLORIDE

≥98% (HPLC)

Synonym(s):

1-(1-(Methylsulfonyl)cyclopropyl)-N-(quinolin-8-ylmethyl)methanamine, 5A6-78, N-[[1-(Methylsulfonyl)cyclopropyl]methyl]-8-quinolinemethanamine

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About This Item

Empirical Formula (Hill Notation):
C15H18N2O2S · xHCl
Molecular Weight:
290.38 (free base basis)
NACRES:
NA.77
UNSPSC Code:
12352200
Assay:
≥98% (HPLC)
Form:
powder
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Quality Segment

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

H2O: 2 mg/mL, clear (Warmed)

storage temp.

-10 to -25°C

Biochem/physiol Actions

Selective, β-arrestin-biased high-affinity 5-HT5A partial agonist. A superior 5-HT5A probe than the non-selective and lower affinity 5-HT5A antagonist SB-699551.
UCSF678 (5A6-78) is a selective, high-affinity (Ki 41.6 nM) β-arrestin-biased 5-HT5A partial agonist (β-arrestin 2 recruitment Emax at 10 μM = 17% of 5-HT Emax) with only off-target affinity toward 1A/2B/7A among >300 GPCRs (>1 μM). UCSF678 is a superior 5-HT5A probe than the non-selective and lower affinity 5-HT5A antagonist SB-699551. The use of UCSF678 shows that 5-HT5AR engagement is nonessential for alleviating pain in a mouse model of peripheral nerve injury-induced mechanical hypersensitivity, which runs contrary to previous studies using less selective ligands.


Storage Class

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable



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