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

Item Number
C107671
Grouped product items
SKUSizeAvailabilityPrice Qty
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
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regulator of G-protein signaling 17 Inhibitor

Basic Description

Synonymscelastrol | 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 & PurityMoligand™, analytical standard, ≥98%
Biochemical and Physiological Mechanisms

Celastrol (Tripterin) is a plant-derived triterpene. Celastrol(Tripterin) has anti-inflammatory and immunosuppressive activity. Celastrol(Tripterin) is Antioxidant and anti-inflammatory agent. Potently inhibits lipid peroxidation in mitoc

Storage TempStore at -20°C
Shipped InIce chest + Ice pads
Gradeanalytical standard, Moligand™
Action TypeINHIBITOR
Mechanism of actionInhibitor 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(Human)

HIF1A Tchem Hypoxia-inducible factor 1-alpha 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

TERT Tchem Telomerase reverse transcriptase 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

RGS17 Tchem Regulator of G-protein signaling 17 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (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 NumberCertificate TypeDateItem
I2116200Certificate of AnalysisJun 14, 2023 C107671
C2218431Certificate of AnalysisMar 24, 2022 C107671
C2218450Certificate of AnalysisMar 24, 2022 C107671

Chemical and Physical Properties

SolubilitySoluble 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

Related Documents

 SDS

 Specification Sheet

Citations of This Product

1. Ping Sheng, Chao Bu, Tanyue Hui, Lili Zhou, Hao Chen, Guoliang Zhou.  (2023)  Polydopamine-activated celastrol carbon dots for synergistic chemotherapy-photothermal therapy of tumors.  International Journal of Pharmaceutics-X,  6  (7): (100218).  [PMID:38033396]
2. Jiwen Fan, Meng Ren, Weiwei Chen, Haodong Wang, Yuquan He.  (2023)  Celastrol relieves myocardial infarction-induced cardiac fibrosis by inhibiting NLRP3 inflammasomes in rats.  INTERNATIONAL IMMUNOPHARMACOLOGY,  121  (110511).  [PMID:37343368]
3. Xiaoli Li, Guangbei Zhu, Xintong Yao, Ning Wang, Ronghui Hu, Qingxin Kong, Duanfang Zhou, Liangyuan Long, Jiali Cai, Weiying Zhou.  (2022)  Celastrol induces ubiquitin-dependent degradation of mTOR in breast cancer cells.  OncoTargets and Therapy,      [PMID:30588010]
4. Qiang Chen, Chunjing Guo, Zhongxin Liu, Min Cao, Wenxin Wang, Dandan Zhang, Hongxu Geng, Ningning Diao, Daquan Chen.  (2023)  Multifunctional nanoparticles with anti-inflammatory effect for improving metabolic syndromes.  JOURNAL OF DRUG TARGETING,  31  (3): (286-295).  [PMID:36315421]
5. Bo Yu, Yiping Shen, Xuejie Zhang, Lijuan Ding, Zheng Meng, Xiaotong Wang, Meihua Han, Yifei Guo, Xiangtao Wang.  (2022)  Poly(methacrylate citric acid) as a Dual Functional Carrier for Tumor Therapy.  Pharmaceutics,  14  (9): (1765).  [PMID:36145512]
6. Yunpeng Qi,Renping Wang,Liang Zhao,Lei Lv,Fan Zhou,Tian Zhang,Feng Lu,Hongli Yan,Gengli Duan.  (2018-08-03)  Celastrol Suppresses Tryptophan Catabolism in Human Colon Cancer Cells as Revealed by Metabolic Profiling and Targeted Metabolite Analysis..  Biological & pharmaceutical bulletin,  41  ((8)): (1243-1250).  [PMID:30068874]

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]
10. Ping Sheng, Chao Bu, Tanyue Hui, Lili Zhou, Hao Chen, Guoliang Zhou.  (2023)  Polydopamine-activated celastrol carbon dots for synergistic chemotherapy-photothermal therapy of tumors.  International Journal of Pharmaceutics-X,  6  (7): (100218).  [PMID:38033396]
11. Jiwen Fan, Meng Ren, Weiwei Chen, Haodong Wang, Yuquan He.  (2023)  Celastrol relieves myocardial infarction-induced cardiac fibrosis by inhibiting NLRP3 inflammasomes in rats.  INTERNATIONAL IMMUNOPHARMACOLOGY,  121  (110511).  [PMID:37343368]
12. Xiaoli Li, Guangbei Zhu, Xintong Yao, Ning Wang, Ronghui Hu, Qingxin Kong, Duanfang Zhou, Liangyuan Long, Jiali Cai, Weiying Zhou.  (2022)  Celastrol induces ubiquitin-dependent degradation of mTOR in breast cancer cells.  OncoTargets and Therapy,      [PMID:30588010]
13. Qiang Chen, Chunjing Guo, Zhongxin Liu, Min Cao, Wenxin Wang, Dandan Zhang, Hongxu Geng, Ningning Diao, Daquan Chen.  (2023)  Multifunctional nanoparticles with anti-inflammatory effect for improving metabolic syndromes.  JOURNAL OF DRUG TARGETING,  31  (3): (286-295).  [PMID:36315421]
14. Bo Yu, Yiping Shen, Xuejie Zhang, Lijuan Ding, Zheng Meng, Xiaotong Wang, Meihua Han, Yifei Guo, Xiangtao Wang.  (2022)  Poly(methacrylate citric acid) as a Dual Functional Carrier for Tumor Therapy.  Pharmaceutics,  14  (9): (1765).  [PMID:36145512]
15. Yunpeng Qi,Renping Wang,Liang Zhao,Lei Lv,Fan Zhou,Tian Zhang,Feng Lu,Hongli Yan,Gengli Duan.  (2018-08-03)  Celastrol Suppresses Tryptophan Catabolism in Human Colon Cancer Cells as Revealed by Metabolic Profiling and Targeted Metabolite Analysis..  Biological & pharmaceutical bulletin,  41  ((8)): (1243-1250).  [PMID:30068874]

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