| Size | Price | |
|---|---|---|
| 1mg | ||
| Other Sizes |
| ln Vitro |
MR 409 (MR-409), as opposed to placebo, dramatically lowers plasma levels of IL-2, IL-6, IL-10, and TNF-α one week after myocardial infarction (MI)[1]. P53 expression in bovine pulmonary artery endothelial cells (BPAECs) is suppressed by MR 409 (MR-409); 1 μM[2]. JAK2, STAT3, and ERK1/2 are activated by MR 409 (1 μM)[2]. PGE2 and 8-iso-PGF2α levels generated by LPS are reduced in a dose-dependent manner by 5 μM[3]. Without demonstrating a dose-dependent impact, MR 409 (1 and 5 μM) reduces LPS-induced lactate dehydrogenase (LDH) activity and nitrite production[3]. Without causing any dose-dependent effects, MR 409 (1 and 5 μM) reduces the gene expression of COX-2, NF-κB, and iNOS that is stimulated by LPS in colon specimens[3]. tMCAO-induced loss of neuroplasticity can be ameliorated and endogenous neurogenesis can be stimulated by MR 409 (MR -409). Additionally, brain stem cells treated with oxygen and glucose deprivation-reperfusion exhibit increased proliferation and inhibited apoptosis in response to MR 409[4].
|
|---|---|
| ln Vivo |
The in vivo growth of lung cancer xenografted into nude mice is inhibited by MR 409 (MR-409)[3]. Mice given daily for 4 weeks with 5 μg of MR 409 show reduced nociceptive response[3].
|
| Cell Assay |
Western Blot Analysis[2]
Cell Types: BPAEC Tested Concentrations: 1 μM Incubation Duration: 24, 48 and 72 hrs (hours) Experimental Results: Dramatically suppressed p53 expression levels after 48 and 72 hrs (hours) of treatment. |
| Animal Protocol |
Animal/Disease Models: Adult C57 /BL6 male mice (5 weeks old, weight 20-22 g)[3]
Doses: 5 µg Route of Administration: Treated daily by subcutaneous (sc) administration of 0.1 mL solution Experimental Results: demonstrated maximal antinociceptive effects at 2 weeks. Sustained a moderate analgesic effect at 4 weeks. |
| References |
| Molecular Formula |
C153H252N44O43
|
|---|---|
| Molecular Weight |
3395.9070148468
|
| Exact Mass |
3394.891
|
| CAS # |
1445155-39-4
|
| PubChem CID |
171361077
|
| Appearance |
White to off-white solid powder
|
| LogP |
-12.3
|
| Hydrogen Bond Donor Count |
52
|
| Hydrogen Bond Acceptor Count |
49
|
| Rotatable Bond Count |
119
|
| Heavy Atom Count |
240
|
| Complexity |
7820
|
| Defined Atom Stereocenter Count |
32
|
| SMILES |
[C@H](C(=O)N[C@@]([H])([C@H](O)C)C(=O)N[C@@H](CC(=O)N)C(=O)N[C@@H](CO)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(=O)N)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](C(=O)NC)CCCNC(N)=N)CC1C=CC(O)=CC=1)(NC(=O)[C@]([H])([C@@H](C)CC)NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@@H](C)NC(=O)[C@@H](NC)CC1C=CC(O)=CC=1)CC1C=CC=CC=1
|
| InChi Key |
JXOVGPGYDSUMMZ-OXEXIPAFSA-N
|
| InChi Code |
InChI=1S/C153H252N44O43/c1-23-27-38-92(129(219)187-108(70-116(208)209)142(232)175-91(125(215)166-22)41-33-58-167-151(159)160)181-148(238)120(80(16)25-3)196-144(234)109(71-117(210)211)188-132(222)98(53-55-113(157)204)180-137(227)100(61-74(5)6)185-138(228)101(62-75(7)8)183-130(220)93(39-31-56-154)176-127(217)95(42-34-59-168-152(161)162)174-122(212)81(17)172-145(235)110(72-198)192-139(229)102(63-76(9)10)184-131(221)97(52-54-112(156)203)179-126(216)90(26-4)173-136(226)103(64-77(11)12)189-147(237)118(78(13)14)194-133(223)94(40-32-57-155)177-128(218)96(43-35-60-169-153(163)164)178-140(230)104(67-87-46-50-89(202)51-47-87)186-146(236)111(73-199)193-141(231)106(68-114(158)205)191-150(240)121(84(20)200)197-143(233)105(66-85-36-29-28-30-37-85)190-149(239)119(79(15)24-2)195-124(214)83(19)171-135(225)107(69-115(206)207)182-123(213)82(18)170-134(224)99(165-21)65-86-44-48-88(201)49-45-86/h28-30,36-37,44-51,74-84,90-111,118-121,165,198-202H,23-27,31-35,38-43,52-73,154-155H2,1-22H3,(H2,156,203)(H2,157,204)(H2,158,205)(H,166,215)(H,170,224)(H,171,225)(H,172,235)(H,173,226)(H,174,212)(H,175,232)(H,176,217)(H,177,218)(H,178,230)(H,179,216)(H,180,227)(H,181,238)(H,182,213)(H,183,220)(H,184,221)(H,185,228)(H,186,236)(H,187,219)(H,188,222)(H,189,237)(H,190,239)(H,191,240)(H,192,229)(H,193,231)(H,194,223)(H,195,214)(H,196,234)(H,197,233)(H,206,207)(H,208,209)(H,210,211)(H4,159,160,167)(H4,161,162,168)(H4,163,164,169)/t79-,80-,81-,82+,83-,84+,90-,91-,92-,93-,94-,95-,96-,97-,98-,99-,100-,101-,102-,103-,104-,105-,106-,107-,108-,109-,110-,111-,118-,119-,120-,121-/m0/s1
|
| Chemical Name |
(3S)-4-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S,3R)-1-[[(2S)-4-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-amino-1-[[(2S)-1-[[(2S,3S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-5-carbamimidamido-1-(methylamino)-1-oxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1-oxohexan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopentan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-1,4-dioxobutan-2-yl]amino]-3-hydroxy-1-oxobutan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-[[(2R)-2-[[(2S)-3-(4-hydroxyphenyl)-2-(methylamino)propanoyl]amino]propanoyl]amino]-4-oxobutanoic acid
|
| 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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.2945 mL | 1.4724 mL | 2.9447 mL | |
| 5 mM | 0.0589 mL | 0.2945 mL | 0.5889 mL | |
| 10 mM | 0.0294 mL | 0.1472 mL | 0.2945 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
