Thapsigargin


Catalog No. Size PriceQuantity
M12335-2 2mg solid $1,230
M12335-10 10mg solid $4,920

Description

Thapsigargin, an endoplasmic reticulum (ER) stress inducer, is an inhibitor of microsomal Ca2+-ATPase. Thapsigargin efficiently inhibits coronavirus (HCoV-229E, MERS-CoV, SARS-CoV-2) replication in different cell types.

Product information

CAS Number: 67526-95-8

Molecular Weight: 650.75

Formula: C34H50O12

Chemical Name: (3S, 3aR, 4S, 6S, 6aR, 7S, 8S, 9bS)-6-(acetyloxy)-4-(butanoyloxy)-3, 3a-dihydroxy-3, 6, 9-trimethyl-8-{[(2Z)-2-methylbut-2-enoyl]oxy}-2-oxo-2H, 3H, 3aH, 4H, 5H, 6H, 6aH, 7H, 8H, 9bH-azuleno[4, 5-b]furan-7-yl octanoate

Smiles: C[C@@]1(O)C(=O)O[C@H]2C3[C@H]([C@H](OC(=O)CCCCCCC)[C@@H](OC(=O)/C(/C)=C\C)C=3C)[C@](C)(C[C@H](OC(=O)CCC)[C@]12O)OC(C)=O

InChiKey: IXFPJGBNCFXKPI-FSIHEZPISA-N

InChi: InChI=1S/C34H50O12/c1-9-12-13-14-15-17-24(37)43-28-26-25(20(5)27(28)44-30(38)19(4)11-3)29-34(41,33(8,40)31(39)45-29)22(42-23(36)16-10-2)18-32(26,7)46-21(6)35/h11,22,26-29,40-41H,9-10,12-18H2,1-8H3/b19-11-/t22-,26+,27-,28-,29-,32-,33+,34+/m0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 100 mg/mL (153.67 mM; Need ultrasonic)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Thapsigargin (0.001- 1 μM; for 2 and 4 days) arrests cell proliferations in MH7A human rheumatoid arthritis synovial cells in a time- and dose-dependent manner. Thapsigargin (0.001- 1 μM; for 2 and 4 days) induces cell apoptosis in MH7A cells in a time- and dose-dependent manner. Thapsigargin (0.001- 1 μM; for 2 and 4 days) impairs mTOR activity and leads to cyclin D1 expressions in MH7A cells. Thapsigargin inhibits Ca2+ entry into human neutrophil granulocytes. Thapsigargin inhibits the carbachol-evoked [Ca2+]i-transients with (IC50=0.353 nM) or without (IC50=0.448 nM) a KCl-prestimulation, but an additional small component, with a much lower sensitivity (IC50=4814 nM), is observed in the absence of a KCl-prestimulation. In contrast, the KCl-evoked [Ca2+]i-transients displayed only one component with a very low sensitivity to Thapsigargin in both absence (IC50=3343 nM) and presence (IC50=6858 nM) of a carbachol-prestimulation.

In Vivo:

Thapsigargin (Injection; 0.25 ug/g, 0.5 ug/g and 1 ug/g; 24 hours) significant increases of 2 to 5-fold in chemokine and pro-inflammatory expression. Thapsigargin is more sensitive to inducing a systemic immune response.

References:

  1. Geiszt M, et al. Thapsigargin inhibits Ca2+ entry into human neutrophil granulocytes. Biochem J. 1995 Jan 15;305 ( Pt 2):525-8.
  2. Wang H, et al. Effects of thapsigargin on the proliferation and survival of human rheumatoid arthritis synovialcells. ScientificWorldJournal. 2014 Feb 9;2014:605416.
  3. Garavito-Aguilar ZV, et al. Differential thapsigargin-sensitivities and interaction of Ca2+ stores in human SH-SY5Y neuroblastoma cells. Brain Res. 2004 Jun 18;1011(2):177-86.

Products are for research use only. Not for human use.

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