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Home > Products > Others > Other > Triptolide (PG490) 38748-32-2

Triptolide (PG490) 38748-32-2

Product Description

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Molecular Weight: 360.4 Triptolide is a diterpene triepoxide, immunosuppresive agent extracted from the Chinese herb Tripterygium wilfordii.
Triptolide is a diterpene triepoxide with potent immunosuppressive and
antiinflammatory properties. Triptolide is shown to inhibit the
expression of IL-2 in activated T cells at the level of
purine-box/nuclear factor and NF-κB mediated transcription activation. Triptolide inhibits the proliferation and colony formation of tumor
cells at extremely low concentrations (2–10 ng/mL). Triptolide has an
inhibitory activity on breast, stomach and leukemia cell line HL-60
cells.


Triptolide induces Apoptosis in tumor cells by blocking NF-κB
activation and sensitizing tumor cells for TNF-&alpha induced
programmed cell death.
Triptolide synergizes with cyclosporin A in promoting graft survival in
animal models and in suppression of graft versus host disease in
allogeneic bone marrow transplants. In addition, it induces apoptosis in
tumor cells and potentiates tumor necrosis factor (TNF-α) induction of
apoptosis in part through the suppression of c-IAP2 and c-IAP1
induction.


Triptolide treatment for 2–3
weeks inhibits the growth of xenografts formed by four different tumor
cell lines (B16 melanoma, MDA-435 breast cancer, TSU bladder cancer, and
MGC80-3 gastric carcinoma), indicating that TPL has a broad spectrum of
activity against tumors that contain both wild-type and mutant forms of
p53. In addition, Triptolide inhibits experimental metastasis of B16F10
cells to the lungs and spleens of mice. Triptolide has in vitro and in vivo activities against mouse models of polycystic kidney disease. LD50: Mice 0.83mg/kg (i.v.).






Protocol(Only for Reference)


Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)


Species Baboon Dog Monkey Rabbit Guinea pig Rat Hamster Mouse
Weight (kg) 12 10 3 1.8 0.4 0.15 0.08 0.02
Body Surface Area (m2) 0.6 0.5 0.24 0.15 0.05 0.025 0.02 0.007
Km factor 20 20 12 12 8 6 5 3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by Animal B Km
Animal A Km



For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) × mouse Km(3) = 11.2 mg/kg
rat Km(6)






Chemical Information




Molecular Weight (MW) 360.4
Formula

C20H24O6

CAS No. 38748-32-2

Storage 3 years -20℃Powder
6 months-80℃in solvent (DMSO, water, etc.)
Synonyms



Solubility (25°C) * In vitro DMSO 72 mg/mL (199.77 mM)
Water <1 mg/mL (
Ethanol <1 mg/mL (





Chemical Name Trisoxireno[4b,5:6,7:8a,9]phenanthro[1,2-c]furan-1(3H)-one, 3b,4,4a,6,6a,7a,7b,8b,9,10-decahydro-6-hydroxy-8b-methyl-6a-(1-methylethyl)-, (3bS,4aS,5aS,6R,6aR,7aS,7bS,8aS,8bS)-







Stock Solution (1ml DMSO) 1mM 10mM 20mM 30mM
Mass(mg) 0.3604 3.604 7.208 10.812


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