Pyr3 - ≥98%, high purity , CAS No.1160514-60-2, Channel blocker of TRPC3

Item Number
P275699
Grouped product items
SKUSizeAvailabilityPrice Qty
P275699-5mg
5mg
In stock
$86.90
P275699-10mg
10mg
In stock
$129.90
P275699-25mg
25mg
In stock
$271.90
P275699-50mg
50mg
In stock
$456.90
P275699-100mg
100mg
In stock
$822.90
P275699-250mg
250mg
In stock
$1,850.90

Selective TRPC3 channel blocker

View related series
TRPC3 Channel blocker

Basic Description

SynonymsJ-003374 | AKOS024457787 | 1-[4-[(2,3,3-Trichloro-1-oxo-2-propen-1-yl)amino]phenyl]-5-(trifluoromethyl)-1H-pyrazole-4-carboxylic acid | CS-0028846 | GTPL4293 | ethyl 1-(4-(2,3,3-trichloroacrylamido)phenyl)-5-(trifluoromethyl)-1h-pyrazole-4-carboxylate | 1
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsSelective TRPC3 channel blocker (IC 50 = 0.7 μM, Ca 2+ influx). Diminishes depolarization in the immature cortex. Blunts BDNF secretion and shows anti-inflammatory effects. Shows neuroprotective effects in vivo.
Storage TempStore at -20°C,Desiccated
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeCHANNEL BLOCKER
Mechanism of actionChannel blocker of TRPC3
NoteWherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description

Store at -20°C. Store under desiccating conditions. The product can be stored for up to 12 months.


General description

Pyr3, a pyrazole compound, selectively inhibits the canonical transient receptor potential channel 3 (TRPC3).

TRPC3 is a member of TRPCs which control influxes of Ca2+ and other cations that induce diverse cellular processes upon stimulation of plasma membrane receptors coupled to phospholipase C. TRPC3 has been implicated in diverse biological functions, including B cell receptor-mediated Ca2+ oscillations, T cell receptor-dependent Ca2+ entry pathway, and cardiac hypertrophy. 

In addition, the transverse aortic constriction operation-induced increase in expression of atrial natriuretic peptide mRNA, a reliable marker for cardiac hypertrophy, was also suppressed by Pyr3.


Associated Targets(Human)

TRPC3 Tchem Short transient receptor potential channel 3 (5 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
TRPV1 Tclin Vanilloid receptor (8273 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
U2OS (164939 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HepG2 (196354 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MDA-MB-231 (73002 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
TRPC3 Tchem Short transient receptor potential channel 3 (70 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HEK-293T (167025 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ORAI1 Tchem ORAI1/STIM1 (242 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ORAI1 Tchem Short transient receptor potential channel 1 & 3/Stromal interaction molecule 1/Calcium release-activated calcium channel protein 1 (72 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ORAI1 Tchem Stromal interaction molecule 1 & 2/Calcium release-activated calcium channel protein 1 (2 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Trpm8 Transient receptor potential cation channel subfamily M member 8 (889 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Trpv1 Transient receptor potential cation channel subfamily V member 1 (45 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

IUPAC Name ethyl 1-[4-(2,3,3-trichloroprop-2-enoylamino)phenyl]-5-(trifluoromethyl)pyrazole-4-carboxylate
INCHI InChI=1S/C16H11Cl3F3N3O3/c1-2-28-15(27)10-7-23-25(12(10)16(20,21)22)9-5-3-8(4-6-9)24-14(26)11(17)13(18)19/h3-7H,2H2,1H3,(H,24,26)
InChi Key RZHGONNSASQOAY-UHFFFAOYSA-N
Canonical SMILES CCOC(=O)C1=C(N(N=C1)C2=CC=C(C=C2)NC(=O)C(=C(Cl)Cl)Cl)C(F)(F)F
Isomeric SMILES CCOC(=O)C1=C(N(N=C1)C2=CC=C(C=C2)NC(=O)C(=C(Cl)Cl)Cl)C(F)(F)F
PubChem CID 56964346
Molecular Weight 456.64

Certificates

Certificate of Analysis(COA)

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8 results found

Lot NumberCertificate TypeDateItem
K2416022Certificate of AnalysisNov 27, 2024 P275699
K2416030Certificate of AnalysisNov 27, 2024 P275699
J2219702Certificate of AnalysisAug 17, 2023 P275699
J2219719Certificate of AnalysisAug 17, 2023 P275699
J2219734Certificate of AnalysisAug 17, 2023 P275699
J2219735Certificate of AnalysisAug 17, 2023 P275699
J2219736Certificate of AnalysisAug 17, 2023 P275699
J2219739Certificate of AnalysisAug 17, 2023 P275699

Chemical and Physical Properties

SolubilitySoluble in DMSO to 75 mM

Related Documents

References

1. Sekerková G et al..  (2013)  Early onset of ataxia in moonwalker mice is accompanied by complete ablation of type II unipolar brush cells and Purkinje cell dysfunction..  J Neurosci,  33  (50): (19689-94).  [PMID:24336732]

Solution Calculators