| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
Kalopanaxsaponin B inhibits Interleukin-1 receptor-associated kinase 1 (IRAK1). It does not inhibit the binding of LPS to TLR4.
Other reported activities include inhibition of acetylcholinesterase (AChE, IC50 = 31.3 μM) and hyaluronidase (IC50 = 280.4 μM), and competitive inhibition of porcine pancreatic elastase (IC50 = 40.6 μM). |
|---|---|
| ln Vitro |
[1] In LPS-stimulated mouse peritoneal macrophages, Kalopanaxsaponin B inhibited the expression of pro-inflammatory mediators TNF-α, IL-1β, iNOS, and COX-2. It also inhibited the activation of IRAK1, IKK-β, NF-κB, and MAP kinases (ERK, JNK, p38). The compound inhibited LPS-induced IRAK1 degradation and phosphorylation.
[1] In a mouse model of TNBS-induced colitis, Kalopanaxsaponin B inhibited the increase in myeloperoxidase (MPO) activity, a marker of neutrophil infiltration. It also inhibited the expression of pro-inflammatory cytokines IL-1β, IL-6, and TNF-α and suppressed NF-κB activation. [1] In a carrageenan-induced hind paw edema model in rats, Kalopanaxsaponin B (0.02 mg/kg) reduced paw edema by 37%. [1] In LPS-challenged mice, Kalopanaxsaponin B (5 mg/kg, i.p.) reduced serum TNF-α and IL-1β levels by 60% and 65%, respectively. [1] Kalopanaxsaponin B has been reported to ameliorate memory deficits in mice by inhibiting AChE activity and inducing BDNF and p-CREB expression. |
| ln Vivo |
[1] IRAK1 kinase binding activity assay: The ability of Kalopanaxsaponin B to inhibit IRAK1 kinase binding activity was measured. The compound did not inhibit NF-κB activation in active IKK-β-transfected macrophages, indicating its specific action is upstream of IKK-β.
[1] The compound did not inhibit the binding of LPS to toll-like receptor 4 (TLR4) on macrophages. [1] Other enzyme inhibition assays: Kalopanaxsaponin B non-competitively inhibits hyaluronidase (IC50 = 280.4 μM) and competitively inhibits porcine pancreatic elastase (IC50 = 40.6 μM). |
| Enzyme Assay |
[1] LPS-stimulated mouse peritoneal macrophages were used to assess the anti-inflammatory effects of Kalopanaxsaponin B. Cells were isolated and treated with LPS in the presence of the compound. The expression of TNF-α, IL-1β, iNOS, and COX-2 was measured.
[1] Active IKK-β-transfected macrophages were used to demonstrate that Kalopanaxsaponin B does not inhibit NF-κB activation downstream of IKK-β. [1] AChE inhibition was measured with an IC50 of 31.3 μM. [1] Antimutagenic activity against aflatoxin B1 was assessed in *S. typhimurium* agar cultures (0.5-5 μg per plate), showing 21-67% inhibition. |
| Cell Assay |
[1] Male ICR mice were used for the LPS-induced systemic inflammation model. Kalopanaxsaponin B was administered intraperitoneally (i.p.).
[1] For the TNBS-induced colitis model, mice were administered TNBS, and the effect of Kalopanaxsaponin B on colon shortening, MPO activity, cytokine expression, and NF-κB activation was assessed. [1] For the carrageenan-induced paw edema model, rats were used. Kalopanaxsaponin B was administered at 0.02 mg/kg. [1] For the memory impairment model, Kalopanaxsaponin B was administered at 40 mg/kg in mice. |
| Animal Protocol |
[1] Kalopanaxsaponin B is metabolized by human intestinal microflora. The main metabolites identified are kalopanaxsaponin A and hederagenin.
|
| Toxicity/Toxicokinetics |
[1] Kalopanaxsaponin B and Kalopanaxsaponin A are the main saponins isolated from the stem bark of *Kalopanax pictus*. They have been shown to exhibit anti-inflammatory, antinociceptive, anti-rheumatoidal, antidiabetic, antimutagenic, and memory-enhancing activities. The compound is a bisdesmoside, and its antimutagenic and cytotoxic activities are structure-dependent.
[1] Kalopanaxsaponin B is for research use only. |
| References |
|
| Additional Infomation |
Kalopana saponin B is a triterpenoid saponin with hederogenin as its aglycone. It has been isolated from the stem bark of Kalopanax pictus. It possesses anti-inflammatory properties and is a plant metabolite. It is a pentacyclic triterpenoid compound, belonging to the class of triterpenoid saponins and carboxylic acid esters. Its function is related to hederogenin. Hederogenin C has also been reported in Eleutherococcus sieboldianus, Caltha palustris, and other organisms with relevant data. See also: Ivy leaves (partial); Hederogenin C (note moved here).
[3] Kalopanaxsaponin B is a natural compound extracted from *Hedera helix* with anti-inflammatory properties. In this study, it protects against AGEs-induced ECM degradation in chondrocytes by suppressing oxidative stress, reducing inflammatory cytokines, and inhibiting NF-κB signaling. It promotes collagen II and aggrecan synthesis and reduces MMP-13 and ADAMTS-5, suggesting its potential as a therapeutic agent for osteoarthritis. [3] |
| Molecular Formula |
C59H96O56
|
|---|---|
| Molecular Weight |
1221.39
|
| Exact Mass |
1220.619
|
| CAS # |
14216-03-6
|
| Related CAS # |
Hederacoside D;760961-03-3
|
| PubChem CID |
11491905
|
| Appearance |
White to off-white solid powder
|
| Density |
1.5±0.1 g/cm3
|
| Melting Point |
222ºC (dec.)(lit.)
|
| Index of Refraction |
1.637
|
| LogP |
4.52
|
| Hydrogen Bond Donor Count |
15
|
| Hydrogen Bond Acceptor Count |
26
|
| Rotatable Bond Count |
14
|
| Heavy Atom Count |
85
|
| Complexity |
2370
|
| Defined Atom Stereocenter Count |
33
|
| SMILES |
C[C@H]1[C@@H]([C@H]([C@H]([C@@H](O1)O[C@@H]2[C@H](O[C@H]([C@@H]([C@H]2O)O)OC[C@@H]3[C@H]([C@@H]([C@H]([C@@H](O3)OC(=O)[C@@]45CC[C@@]6(C(=CC[C@H]7[C@]6(CC[C@@H]8[C@@]7(CC[C@@H]([C@@]8(C)CO)O[C@H]9[C@@H]([C@H]([C@H](CO9)O)O)O[C@H]1[C@@H]([C@@H]([C@H]([C@@H](O1)C)O)O)O)C)C)[C@@H]4CC(CC5)(C)C)C)O)O)O)CO)O)O)O
|
| InChi Key |
RYHDIBJJJRNDSX-MCGLQMIESA-N
|
| InChi Code |
InChI=1S/C59H96O26/c1-24-34(63)38(67)42(71)49(78-24)83-46-29(20-60)80-48(45(74)41(46)70)77-22-30-37(66)40(69)44(73)51(81-30)85-53(75)59-17-15-54(3,4)19-27(59)26-9-10-32-55(5)13-12-33(56(6,23-61)31(55)11-14-58(32,8)57(26,7)16-18-59)82-52-47(36(65)28(62)21-76-52)84-50-43(72)39(68)35(64)25(2)79-50/h9,24-25,27-52,60-74H,10-23H2,1-8H3/t24-,25-,27-,28-,29+,30+,31+,32+,33-,34-,35-,36-,37+,38+,39+,40-,41+,42+,43+,44+,45+,46+,47+,48+,49-,50-,51-,52-,55-,56-,57+,58+,59-/m0/s1
|
| Chemical Name |
Olean-12-en-28-oic acid, 3- ((2-O-(6-deoxy-alpha-L-mannopyranosyl)-alpha-L-arabinopyranosyl)oxy)-23-hydroxy-, O-6-deoxy-alpha-L-mannopyranosyl-(1-4)-O-beta-D-glucopyranosyl-(1-6)-beta-D-glucopyranosyl ester, (3beta,4alpha)-
|
| Synonyms |
Hederacoside C Hederoside H1Glycoside L-H2Kalopanaxsaponin B
|
| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~81.87 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.05 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (2.05 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (2.05 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.8187 mL | 4.0937 mL | 8.1874 mL | |
| 5 mM | 0.1637 mL | 0.8187 mL | 1.6375 mL | |
| 10 mM | 0.0819 mL | 0.4094 mL | 0.8187 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
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