ethyl 5-((1-methyl-4-nitro-1H-imidazol-5-yl)oxy)-2-phenylbenzofuran-3-carboxylate

Product Nameethyl 5-((1-methyl-4-nitro-1H-imidazol-5-yl)oxy)-2-phenylbenzofuran-3-carboxylate
CAS300803-69-4
MFC21H17N3O6
MW407.38
EINECS
MOL File300803-69-4.mol

Chemical Properties

storage temp.	Store at -20°C
solubility	Soluble in DMSO
form	A solid
color	White to off-white
InChIKey	UJHGRDVYTTVJFD-UHFFFAOYSA-N
SMILES	[N+](=O)([O-])c1nc[n](c1Oc2cc3c([o]c(c3C(=O)OCC)c4ccccc4)cc2)C

Safety Information

WGK Germany	WGK 3
Storage Class	13 - Non Combustible Solids

Usage And Synthesis

Uses

OB-1 is a stomatin-like protein-3 (STOML3) oligomerization blocker. OB-1 is an effective inhibitor of the self-association of Stomatin, STOML1 and STOML2, but not podocin[1].

Biological Activity

OB-1 is an inhibitor of the oligomerization of Stomatin-like protein-3 (STOML3), which is a modulator of the mechanosensitive ion channel Piezo2. STOML3 requires oligomerization for its role as an endogenous regulator of the sensitivity of mechanosensitive Piezo ion channels in sensory neurons. By inhibiting this activity, OB-1 has been shown to reduce touch-evoked pain behavior in two mouse models of neuropathic pain.

in vivo

OB-1 (250-500 pmol per paw; s.c.; once) reversibly reduces the sensitivity of mechanically gated currents in sensory neurons and silence mechanoreceptors in mice^[1].
OB-1 (250 pmol per paw; s.c.; once) alleviates painful diabetic neuropathy in mice^[1].

Animal Model:	C57Bl/6N mice^[1]
Dosage:	250-500 pmol per paw
Administration:	Subcutaneous injection, once
Result:	Over 40% of Aβ fibers (19/44) lacked a mechanosensitive receptive field, which was significantly different from that in vehicle-injected controls, where less than 7% (5/69 fibers) were found to be insensitive to mechanical stimuli. Reduced touch perception. Reversed tactile allodynia.

Animal Model:	Eight-week-old C57Bl/6 mice, Streptozotocin (HY-13753) model^[1]
Dosage:	250 pmol per paw
Administration:	Subcutaneous injection, once
Result:	Substantially reversed the mechanical hypersensitivity 4 h after treatment.

storage

Store at RT

References

[1] Wetzel C, et al. Small-molecule inhibition of STOML3 oligomerization reverses pathological mechanical hypersensitivity. Nat Neurosci. 2017 Feb;20(2):209-218. DOI:10.1038/nn.4454

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