| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
|
LMD-009 (LMD009) is a novel and potent nonpeptide CCR8 agonist with anti-inflammatory activity. LMD-009 selectively stimulated CCR8 among the 20 identified human chemokine receptors. It mediated chemotaxis, inositol phosphate accumulation, and calcium release with high potencies (EC50 from 11 to 87 nM) and with efficacies similar to that of the endogenous agonist CCL1, and it competed for 125I-CCL1 binding with an affinity of 66 nM.
| ln Vitro |
In harvested COS-7 cells expressing human CCR8, LMD-009 (0 -20 nM; 90 min) increases the formation of phosphoinositides [1]. LMD-009 (0-100 nM; 90 min) 1 h) mediates LMD-009 (0.1 nM-100 μM; 40 min)-induced migration of L1.2 cells [1]. LMD-009 (0–10 μM; 90 min) releases calcium from COS-Chinese hamster ovarian cells [1]. Other human chemokine receptors are not antagonistically active to LMD-009 (0-10 nM; 90 min) [1]. Molecular reactions in 7 cells deviate from CCR8 mutations [1].
|
|---|---|
| Cell Assay |
Cell Viability Assay[1]
Cell Types: COS-7 cells Tested Concentrations: 0-20 nM Incubation Duration: 90 minutes Experimental Results: Stimulates the accumulation of phosphoinositide in COS-7 cells expressing human CCR8 receptor with an EC50 value of 11 nM. Does not inhibit any receptors of other human chemokine receptors. Cell viability assay [1] Cell Types: Chinese hamster ovary cells Tested Concentrations: 0-100 nM Incubation Duration: 1 hour Experimental Results: Calcium release from Chinese hamster ovary cells is regulated, EC50 value is 87 nM. Cell migration assay [1] Cell Types: Lymphocyte L1.2 cells. Tested Concentrations: 0.1 nM- 100 μM Incubation Duration: 40 minutes Experimental Results: The Ki value of L1.2 cells is 66 nM, and it specifically binds 125I-CCL1. |
| References |
| Molecular Formula |
C29H33N3O3
|
|---|---|
| Molecular Weight |
471.59062743187
|
| Exact Mass |
471.252
|
| CAS # |
950195-51-4
|
| PubChem CID |
91032188
|
| Appearance |
White to off-white solid powder
|
| LogP |
4.8
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
35
|
| Complexity |
674
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C1C2(CCN(CC3C=C(OC4C(OC)=CC=CC=4)C=CC=3)CC2)N(CCC2C=CC=CC=2)CN1
|
| InChi Key |
MRXASGVUQJVWMP-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C29H33N3O3/c1-34-26-12-5-6-13-27(26)35-25-11-7-10-24(20-25)21-31-18-15-29(16-19-31)28(33)30-22-32(29)17-14-23-8-3-2-4-9-23/h2-13,20H,14-19,21-22H2,1H3,(H,30,33)
|
| Chemical Name |
8-[[3-(2-methoxyphenoxy)phenyl]methyl]-1-(2-phenylethyl)-1,3,8-triazaspiro[4.5]decan-4-one
|
| HS Tariff Code |
2934.99.9001
|
| 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 : ~250 mg/mL (~530.12 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.41 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 20.8 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: ≥ 2.08 mg/mL (4.41 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 20.8 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: ≥ 2.08 mg/mL (4.41 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 | 2.1205 mL | 10.6024 mL | 21.2049 mL | |
| 5 mM | 0.4241 mL | 2.1205 mL | 4.2410 mL | |
| 10 mM | 0.2120 mL | 1.0602 mL | 2.1205 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
Copyright 2020 InvivoChem LLC | All Rights Reserved
