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Celastrol - analytical standard，≥98%, high purity , CAS No.34157-83-0, Inhibitor of regulator of G-protein signaling 17

analytical standard
Moligand™
≥98%

CAS#: 34157-83-0
Formula: C₂₉H₃₈O₄
Molecular Weight: 450.61
EC Number: 636-472-5
MDL number: MFCD03424073
PubChem CID: 122724

Item Number

C107671

Grouped product items
SKU	Size	Availability	Price
C107671-10mg	10mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$130.90
C107671-20mg	20mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$237.90
C107671-50mg	50mg	Available within 4-8 weeks(?) Items will be manufactured post-order and can take 4-8 weeks. Thank you for your patience!	$1,241.90

View related series

regulator of G-protein signaling 17 Inhibitor

Basic Description

Synonyms	celastrol\|34157-83-0\|Tripterin\|Tripterine\|(2R,4aS,6aS,12bR,14aS,14bR)-10-hydroxy-2,4a,6a,9,12b,14a-hexamethyl-11-oxo-1,2,3,4,4a,5,6,6a,11,12b,13,14,14a,14b-tetradecahydropicene-2-carboxylic acid\|NSC70931\|(2R,4aS,6aR,6aS,14aS,14bR)-10-hydroxy-2,4a,6a,6a,9,
Specifications & Purity	analytical standard，≥98%
Storage Temp	Store at -20°C
Shipped In	Dry ice
Grade	analytical standard, Moligand™
Action Type	INHIBITOR
Mechanism of action	Inhibitor of regulator of G-protein signaling 17
Product Description	Celastrol, Celastrus scandens, a compound originally purified from Tripterygium wilfordii, has been shown to be an anti-peroxidative and anti-angiogenic agent. Mechanistic studies suggest that Celastrol suppresses levels of VEGF and Flk-1 receptors, VEGFR-1 and VEGFR-2, which may reduce signal transduction between the two growth factors. Additionally, Celastrol has demonstrated the ability to disrupt critical interaction of Glu33 (Hsp90) and Arg167 (Cdc37) in the superchaperone complex which causes anti-proliferative activity in vitro and inhibit Topo II (topoisomerase II) activity in vitro (IC50 = 7.41 μM). Celastrol, Celastrus scandens is an inhibitor of Hsp90.

Associated Targets

HIF1A Tchem Hypoxia-inducible factor 1-alpha 1 Activities

Discover Target: HIF1A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

TERT Tchem Telomerase reverse transcriptase 1 Activities

Discover Target: TERT

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

RGS17 Tchem Regulator of G-protein signaling 17 0 Activities

Discover Target: RGS17

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Names and Identifiers

IUPAC Name	(2R,4aS,6aR,6aS,14aS,14bR)-10-hydroxy-2,4a,6a,6a,9,14a-hexamethyl-11-oxo-1,3,4,5,6,13,14,14b-octahydropicene-2-carboxylic acid
INCHI	InChI=1S/C29H38O4/c1-17-18-7-8-21-27(4,19(18)15-20(30)23(17)31)12-14-29(6)22-16-26(3,24(32)33)10-9-25(22,2)11-13-28(21,29)5/h7-8,15,22,31H,9-14,16H2,1-6H3,(H,32,33)/t22-,25-,26-,27+,28-,29+/m1/s1
InChi Key	KQJSQWZMSAGSHN-JJWQIEBTSA-N
Canonical SMILES	CC1=C(C(=O)C=C2C1=CC=C3C2(CCC4(C3(CCC5(C4CC(CC5)(C)C(=O)O)C)C)C)C)O
Isomeric SMILES	CC1=C(C(=O)C=C2C1=CC=C3[C@]2(CC[C@@]4([C@@]3(CC[C@@]5([C@H]4C[C@](CC5)(C)C(=O)O)C)C)C)C)O
WGK Germany	2
Alternate CAS	34157-83-0
PubChem CID	122724
NSC Number	70931
UN Number	2811
MeSH Entry Terms	3-hydroxy-24-nor-2-oxo-1(10),3,5,7-friedelatetraen-29-oic acid;celastrol;tripterin;tripterine
Molecular Weight	450.61

Certificates

Certificate of Analysis(COA)

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3 results found

Lot Number	Certificate Type	Date	Item
I2116200	Certificate of Analysis	Jun 14, 2023	C107671
C2218431	Certificate of Analysis	Mar 24, 2022	C107671
C2218450	Certificate of Analysis	Mar 24, 2022	C107671

Solubility

Soluble in DMSO (>10 mg/ml), ethanol, DMF:PBS(pH 7.2)(1:10), and DMF. Insoluble in water.

Specific Rotation[α]

-122.7° (C=0.1,CHCl3)

Melt Point(°C)

203°C(lit.)

Safety and Hazards(GHS)

Pictogram(s)	GHS06
Signal	Danger
Hazard Statements	H301:Toxic if swallowed
Precautionary Statements	P321:Specific treatment (see ... on this label). P405:Store locked up. P501:Dispose of contents/container to ... P264:Wash hands [and …] thoroughly after handling. P270:Do not eat, drink or smoke when using this product. P330:Rinse mouth. P301+P316:IF SWALLOWED: Get emergency medical help immediately.
WGK Germany	2

References

1. Allison AC, Cacabelos R, Lombardi VR, Alvarez XA, Vigo C. (2001) Celastrol, a potent antioxidant and anti-inflammatory drug, as a possible treatment for Alzheimer's disease.. Prog Neuropsychopharmacol Biol Psychiatry, 25 (7): (1341-57). [PMID:11513350]
2. Pfuhlmann K, Schriever SC, Baumann P, Kabra DG, Harrison L, Mazibuko-Mbeje SE, Contreras RE, Kyriakou E, Simonds SE, Tiganis T et al.. (2018) Celastrol-Induced Weight Loss Is Driven by Hypophagia and Independent From UCP1.. Diabetes, 67 (11): (2456-2465). [PMID:30158241]
3. Zhan X, Yan C, Chen Y, Wei X, Xiao J, Deng L, Yang Y, Qiu P, Chen Q. (2018) Celastrol antagonizes high glucose-evoked podocyte injury, inflammation and insulin resistance by restoring the HO-1-mediated autophagy pathway.. Mol Immunol, 104 (3): (61-68). [PMID:30439604]
4. Wong VKW, Qiu C, Xu SW, Law BYK, Zeng W, Wang H, Michelangeli F, Dias IRSR, Qu YQ, Chan TW et al.. (2019) Ca²⁺ signalling plays a role in celastrol-mediated suppression of synovial fibroblasts of rheumatoid arthritis patients and experimental arthritis in rats.. Br J Pharmacol, 176 (16): (2922-2944). [PMID:31124139]
5. Shi K, Chen X, Xie B, Yang SS, Liu D, Dai G, Chen Q. (2018) Celastrol Alleviates Chronic Obstructive Pulmonary Disease by Inhibiting Cellular Inflammation Induced by Cigarette Smoke via the Ednrb/Kng1 Signaling Pathway.. Front Pharmacol, 9 (3): (1276). [PMID:30498444]
6. Zhang J, Zhou K, Zhang X, Zhou Y, Li Z, Shang F. (2019) Celastrol Ameliorates Inflammation in Human Retinal Pigment Epithelial Cells by Suppressing NF-κB Signaling.. J Ocul Pharmacol Ther, 35 (2): (116-123). [PMID:30596540]
7. Zhou X, Cao X, Tu H, Zhang ZR, Deng L. (2019) Inflammation-Targeted Delivery of Celastrol via Neutrophil Membrane-Coated Nanoparticles in the Management of Acute Pancreatitis.. Mol Pharm, 16 (3): (1397-1405). [PMID:30753778]
8. Venkatesha SH, Moudgil KD. (2019) Celastrol suppresses experimental autoimmune encephalomyelitis via MAPK/SGK1-regulated mediators of autoimmune pathology.. Inflamm Res, 68 (4): (285-296). [PMID:30820608]
9. Feng X, Guan D, Auen T, Choi JW, Salazar Hernández MA, Lee J, Chun H, Faruk F, Kaplun E, Herbert Z et al.. (2019) IL1R1 is required for celastrol's leptin-sensitization and antiobesity effects.. Nat Med, 25 (4): (575-582). [PMID:30833749]

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