2. Membrane Transporter/Ion Channel Neuronal Signaling GPCR/G Protein Metabolic Enzyme/Protease Apoptosis Immunology/Inflammation
  3. Calcium Channel Platelet-activating Factor Receptor (PAFR) UGT Leukotriene Receptor TNF Receptor PGE synthase Interleukin Related
  4. Yangambin

Yangambin is a PAF receptor antagonist and UGT1A1/UGT1A3 inhibitor, with an IC50 of 29.7 μM and a Ki of 17.1 μM against human UGT1A1, and an IC50 of 56.5 μM and a Ki of 66.8 μM against human UGT1A3. Yangambin blocks PAF-mediated responses, inhibits LTB4-mediated neutrophil infiltration, and suppresses inflammatory events and anaphylactic contraction. Yangambin acts as a central nervous system inhibitor to reduce spontaneous activity, and also exhibits analgesic, anticonvulsant, antileishmanial, vasodilatory and hypotensive effects. Yangambin blocks voltage-gated Ca2+ channels, reduces the production of NO, TNF-α, IL-6 and PGE2 in cells, increases the production of IL-10, and exerts a protective effect against cardiovascular injury. Yangambin can be used in research related to allergies, cutaneous leishmaniasis, central nervous system diseases and cardiovascular diseases.

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Yangambin

Yangambin Chemical Structure

CAS No. : 13060-14-5

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Based on 1 publication(s) in Google Scholar

Yangambin Related Antibodies

Top Publications Citing Use of Products

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

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LTB4 LTC4/CysLT2 LTD4/CysLT1 LTE4

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TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF10B/DR5/CD262 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

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  • Purity & Documentation

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Description

Yangambin is a PAF receptor antagonist and UGT1A1/UGT1A3 inhibitor, with an IC50 of 29.7 μM and a Ki of 17.1 μM against human UGT1A1, and an IC50 of 56.5 μM and a Ki of 66.8 μM against human UGT1A3. Yangambin blocks PAF-mediated responses, inhibits LTB4-mediated neutrophil infiltration, and suppresses inflammatory events and anaphylactic contraction. Yangambin acts as a central nervous system inhibitor to reduce spontaneous activity, and also exhibits analgesic, anticonvulsant, antileishmanial, vasodilatory and hypotensive effects. Yangambin blocks voltage-gated Ca2+ channels, reduces the production of NO, TNF-α, IL-6 and PGE2 in cells, increases the production of IL-10, and exerts a protective effect against cardiovascular injury. Yangambin can be used in research related to allergies, cutaneous leishmaniasis, central nervous system diseases and cardiovascular diseases[1][2][3][4][5][6].

IC50 & Target[6][3][1]

UGT1A1

29.7 μM (IC50)

UGT1A3

56.5 μM (IC50)

UGT1A1

17.1 μM (Ki)

UGT1A3

66.8 μM (Ki)

IL-6

 

IL-10

 

LTB4

 

Cellular Effect
Cell Line Type Value Description References
BV-2 IC50
28.6 μM
Compound: 3
Inhibition of NO production in LPS-stimulated mouse BV2 cells assessed as nitrite accumulation after 20 hrs by Griess reagent method
Inhibition of NO production in LPS-stimulated mouse BV2 cells assessed as nitrite accumulation after 20 hrs by Griess reagent method
[PMID: 19110419]
In Vitro

Yangambin (50-200 μM; 48 h) potently reduces the viability and survival rate of Leishmania amazonensis in bone marrow-derived macrophages from BALB/c mice, with IC50 values of 43.9 μM and 76 μM, respectively[3].
Yangambin (100 μM; 48 h) reduces the production of NO, TNF-α, IL-6 and PGE2, and increases the production of IL-10, in bone marrow-derived macrophages from BALB/c mice infected with Leishmania amazonensis and stimulated with IFN-γ[3].
Yangambin (0.1 μM-1 mM; pre-incubated prior to 60 mM K+Cl− stimulation) inhibits K+Cl−-induced intracellular calcium signals in Fura-2/AM (HY-101897)-loaded rat mesenteric artery smooth muscle cells in a concentration-dependent manner, with significant inhibitory effects observed at concentrations of 30 μM and 1 mM[5].
Yangambin (0.1-200 µM; 60 min) inhibits the activities of UGT1A1 and UGT1A3 in pooled human liver microsomes, with IC50 values of 29.7 µM and 56.5 µM, respectively[6].
Yangambin (2-40 µM; 30 min) non-competitively inhibits UGT1A1-catalyzed glucuronidation of SN-38 in pooled human liver microsomes, with a Ki value of 17.1 µM[6].
Yangambin (5-80 µM; 30 min) competitively inhibits UGT1A3-catalyzed 24-acyl glucuronidation of chenodeoxycholic acid in pooled human liver microsomes, with a Ki value of 66.8 µM[6].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Yangambin Related Antibodies

Cell Viability Assay[3]

Cell Line: BALB/c mouse BMDM infected with Leishmania amazonensis (MHOM/Br88/Ba-125)
Concentration: 50, 100, 200 μM
Incubation Time: 48 h
Result: Reduced intracellular Leishmania amazonensis viability in a concentration-dependent manner.
Caused a significant reduction in parasite burden at 200 μM, with an IC50 value of 43.9 μM.
Caused a significant reduction in parasite burden at 200 μM, with an IC50 value of 76 μM.
In Vivo

Yangambin (10-20 mg/kg; i.p.; single administration 1 hour prior to challenge) significantly inhibits antigen-induced pleural neutrophil and eosinophil infiltration in sensitized rats, but exerts no inhibitory effect on exudation, and suppresses thrombocytopenia[1].
Yangambin (10-20 mg/kg; i.p.; single administration 1 hour prior to challenge) significantly inhibits platelet-activating factor (PAF)-induced pleural eosinophil accumulation in normal rats. At the dose of 20 mg/kg, it inhibits PAF-induced neutrophil infiltration, but has no effect on exudation, partially inhibits hemoconcentration and leukocytosis, and almost completely blocks thrombocytopenia[1].
Yangambin (20 mg/kg; i.p.; single administration 1 hour prior to challenge) significantly inhibits LTB4 (HY-107608)-induced pleural neutrophil infiltration in normal rats[1].
Yangambin (12.5-50 mg/kg; i.p.; single administration) exerts central nervous system depressant activity in healthy male Swiss mice, reduces spontaneous and upright locomotor activities, prolongs immobility time in the forced swimming test, and alters parameters of the elevated plus maze; it also shortens pentobarbital sleep latency and prolongs pentobarbital-induced sleep duration[2].
Yangambin (10-20 mg/kg; i.v.; single bolus) dose-dependently and selectively inhibits PAF-induced cardiovascular changes and thrombocytopenia in anesthetized rabbits[4].
Yangambin (1-30 mg/kg; i.v.) induces dose-dependent hypotension and tachycardia in normotensive, unanesthetized male Wistar rats[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Wistar (both sexes, 150-200 g, sensitized subcutaneously with Ovalbumin (HY-W250978) + aluminium hydroxide)[1]
Dosage: 10 mg/kg; 20 mg/kg/5 mg/kg; 10 mg/kg; 20 mg/kg
Administration: i.p.; single dose 1 h pre-challenge
Result: Failed to modify antigen-induced pleural exudation.
Significantly inhibited antigen-induced neutrophil infiltration at 4 hours at both 10 and 20 mg/kg.
Significantly inhibited antigen-induced eosinophil accumulation at 24 hours at both 10 and 20 mg/kg.
Failed to modify antigen-induced increases in hematocrit and circulating leucocyte numbers at any dose.
Dose-dependently inhibited antigen-induced thrombocytopenia at 5, 10, and 20 mg/kg.
Animal Model: Wistar (both sexes, 150-200 g)[1]
Dosage: 10 mg/kg; 20 mg/kg
Administration: i.p.; single dose 1 hour pre-challenge
Result: Failed to modify PAF-induced pleural exudation at either dose.
Significantly inhibited PAF-induced eosinophil accumulation at 24 hours at both 10 and 20 mg/kg.
Significantly inhibited PAF-induced neutrophil infiltration at 6 hours only at the 20 mg/kg dose.
Partially inhibited PAF-induced increases in hematocrit and circulating leucocyte numbers at both 10 and 20 mg/kg.
Almost entirely prevented PAF-induced thrombocytopenia at both 10 and 20 mg/kg.
Animal Model: Wistar (both sexes, 150-200 g)[1]
Dosage: 20 mg/kg
Administration: i.p.; single dose 1 hour pre-challenge
Result: Reduced LTB4-induced neutrophil accumulation from 1.42 × 106 cells/cavity to 0.61 × 106 cells/cavity.
Animal Model: Swiss mice (adult male, 25-30 g)[2]
Dosage: 12.5 mg/kg; 25 mg/kg; 50 mg/kg
Administration: i.p.; single dose
Result: Reduced time of permanence in open arms to 63.5 s and 53.2 s, and percentage of time in open arms to 26.7% and 22.6% at 25 mg/kg and 50 mg/kg, respectively.
Reduced rearing to 7.6 and grooming to 1.5 at 12.5 mg/kg; reduced crossed squares to 35.0 and rearing to 6.5 at 25 mg/kg; reduced crossed squares to 29.8, rearing to 5.6, and grooming to 1.4 at 50 mg/kg.
Showed no significant changes in number of falls or time of permanence on the bar at any dose.
Reduced sleep latency to 177.0 s and prolonged sleeping time to 59.7 min at 50 mg/kg; no significant effects at 25 mg/kg.
Increased immobility time to 166.4 s and 187.6 s at 25 mg/kg and 50 mg/kg, respectively.
Animal Model: New Zealand white (either sex, 2-3 kg, pentobarbitone-anaesthetized)[4]
Dosage: 10 mg/kg; 20 mg/kg
Administration: i.v.; single bolus
Result: Attenuated PAF (3.0 μg/kg)-induced mean arterial pressure (MAP) decrease from 49% to 30%, fully prevented PAF-induced bradycardia, and reduced PAF-induced platelet level reduction from 50% to 20% at 10 mg/kg.
Attenuated PAF (3.0 μg/kg)-induced MAP decrease from 49% to 13%, fully prevented PAF-induced bradycardia, and reduced PAF-induced platelet level reduction from 50% to 0.4% at 20 mg/kg.
Caused a short-lasting intrinsic hypotensive effect: 9.5% MAP reduction at 10 mg/kg, 23% MAP reduction at 20 mg/kg.
Failed to inhibit PAF-induced leukopaenia; PAF still caused a 62% reduction in circulating leukocytes at 10 mg/kg and 42% reduction at 20 mg/kg.
Did not alter hypotensive responses to acetylcholine, histamine, 5-hydroxytryptamine, or the hypertensive response to noradrenaline at 10 mg/kg.
Animal Model: Wistar (male, 300-350 g)[5]
Dosage: 1 mg/kg; 5 mg/kg; 10 mg/kg; 20 mg/kg; 30 mg/kg
Administration: i.v.
Result: Induced short-lasting hypotension relative to baseline at each dose: -3.5%, -7.1%, -8.9%, -14%, and -25.5%, respectively.
Induced tachycardia relative to baseline at each dose: 5.9%, 5.9%, 8.8%, 11.6%, and 18.8%, respectively.
Molecular Weight

446.49

Formula

C24H30O8
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

COC1=C(OC)C(OC)=CC([C@H]2OC[C@]3([H])[C@@H](C4=CC(OC)=C(OC)C(OC)=C4)OC[C@@]32[H])=C1
Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (111.98 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2397 mL 11.1985 mL 22.3969 mL
5 mM 0.4479 mL 2.2397 mL 4.4794 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.25 mg/mL (2.80 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 1.25 mg/mL (2.80 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2397 mL 11.1985 mL 22.3969 mL 55.9923 mL
5 mM 0.4479 mL 2.2397 mL 4.4794 mL 11.1985 mL
10 mM 0.2240 mL 1.1198 mL 2.2397 mL 5.5992 mL
15 mM 0.1493 mL 0.7466 mL 1.4931 mL 3.7328 mL
20 mM 0.1120 mL 0.5599 mL 1.1198 mL 2.7996 mL
25 mM 0.0896 mL 0.4479 mL 0.8959 mL 2.2397 mL
30 mM 0.0747 mL 0.3733 mL 0.7466 mL 1.8664 mL
40 mM 0.0560 mL 0.2800 mL 0.5599 mL 1.3998 mL
50 mM 0.0448 mL 0.2240 mL 0.4479 mL 1.1198 mL
60 mM 0.0373 mL 0.1866 mL 0.3733 mL 0.9332 mL
80 mM 0.0280 mL 0.1400 mL 0.2800 mL 0.6999 mL
100 mM 0.0224 mL 0.1120 mL 0.2240 mL 0.5599 mL
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Yangambin Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Yangambin13060-14-5Calcium ChannelPlatelet-activating Factor Receptor (PAFR)UGTLeukotriene ReceptorTNF ReceptorPGE synthaseInterleukin RelatedCa2+ channelsCa channelsUDP-glucuronosyltransferaseUridine diphosphate glucuronosyltransferaseTumor Necrosis Factor ReceptorTNFRProstaglandin E synthaseILhuman liver microsomesLeishmania amazonensisLTB4 receptorUGT1A1PAF receptorrabbit plateletsUGT1A3Leishmania braziliensisBALB/c mouse bone-marrow derived macrophagesrat mesenteric artery smooth muscle cellsInhibitorinhibitorinhibit

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