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| 100mg |
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| 500mg |
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| 1g |
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| 2g |
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| 5g |
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| 10g |
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Purity: ≥98%
Norepinephrine bitartrate (Levarterenol; L-Noradrenaline) is a potent and β1-selective adrenergic receptor agonist with EC50 of 5.37 μM. Norepinephrine is an organic chemical in the catecholamine family that functions in the brain and body as a hormone and neurotransmitter. It is a naturally occurring chemical in the body that acts as both a stress hormone and neurotransmitter (a substance that sends signals between nerve cells). It's released into the blood as a stress hormone when the brain perceives that a stressful event has occurred.
| Targets |
α1-adrenergic receptor; α2-adrenergic receptor; Beta-1 adrenergic receptor
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|---|---|
| ln Vitro |
It is commonly accepted that norepinephrine tartrate (Levarterenol; L-norepinephrine) selectively binds to beta1 subtype adrenergic receptors rather than beta2 adrenergic receptors. At greater concentrations, norepinephrine tartrate (NE) also directly activates β2-adrenergic receptors [2]. From newborn wild-type C57BL/6J mice, adipocytes were extracted and cultivated from the inguinal fat pad (iWA) or the interscapular fat pad (BA). In order to investigate the impact of AT2 activation on β-adrenergic signaling, cAMP responses to norepinephrine (10 µM) were evaluated in the presence or absence of co-administration of CGP (10 nM). In iWA, norepinephrine (NE) increased cAMP as predicted; CGP had no influence on this rise. Additionally, norepinephrine (NE) causes lipolysis, which releases fatty acids required for UCP1 protein activation and thermogenesis promotion. Norepinephrine (NE) treatment in mice with iWA resulted in an increase in the phosphorylation of CREB site Ser133, but CGP combination therapy dramatically decreased it [3].
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| Enzyme Assay |
Beta adrenergic receptors (βARs) mediate physiologic responses to the catecholamines epinephrine and norepinephrine released by the sympathetic nervous system. While the hormone epinephrine binds β1AR and β2AR with similar affinity, the smaller neurotransmitter norepinephrine is approximately tenfold selective for the β1AR. To understand the structural basis for this physiologically important selectivity, we solved the crystal structures of the human β1AR bound to an antagonist carazolol and different agonists including norepinephrine, epinephrine and BI-167107. Structural comparison revealed that the catecholamine-binding pockets are identical between β1AR and β2AR, but the extracellular vestibules have different shapes and electrostatic properties. Metadynamics simulations and mutagenesis studies revealed that these differences influence the path norepinephrine takes to the orthosteric pocket and contribute to the different association rates and thus different affinities [4].
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| Cell Assay |
RT-PCR[2]
Cell Types: subcutaneous preadipocyte adipocyte. Tested Concentrations: 10μM. Incubation Duration: 6 hrs (hours). Experimental Results: AT2 activation inhibits norepinephrine-induced UCP1 in white adipocytes (iWA) |
| References |
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| Molecular Formula |
C12H17NO9
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|---|---|
| Molecular Weight |
319.26468
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| Exact Mass |
319.09
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| Elemental Analysis |
C, 45.14; H, 5.37; N, 4.39; O, 45.10
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| CAS # |
51-40-1
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| Related CAS # |
Norepinephrine;51-41-2;Norepinephrine hydrochloride;329-56-6;Norepinephrine bitartrate monohydrate;108341-18-0; 69815-49-2
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| PubChem CID |
11957447
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| Appearance |
White to off-white solid
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| Boiling Point |
442.6ºC at 760 mmHg
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| Flash Point |
221.5ºC
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| Hydrogen Bond Donor Count |
8
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
22
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| Complexity |
276
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C1=CC(=C(C=C1[C@H](CN)O)O)O.[C@@H]([C@H](C(=O)O)O)(C(=O)O)O
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| InChi Key |
WNPNNLQNNJQYFA-YIDNRZKSSA-N
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| InChi Code |
InChI=1S/C8H11NO3.C4H6O6/c9-4-8(12)5-1-2-6(10)7(11)3-55-1(3(7)8)2(6)4(9)10/h1-3,8,10-12H,4,9H21-2,5-6H,(H,7,8)(H,9,10)/t8-1-,2-/m01/s1
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| Chemical Name |
(R)-4-(2-amino-1-hydroxyethyl)benzene-1,2-diol (2R,3R)-2,3-dihydroxysuccinate
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| Synonyms |
Norepinephrine bitartrate l-Noradrenaline d-bitartrate NSC 169106 NSC-169106 NSC169106
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| 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)
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| Solubility (In Vitro) |
DMSO: >10 mM
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| 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 | 3.1322 mL | 15.6612 mL | 31.3224 mL | |
| 5 mM | 0.6264 mL | 3.1322 mL | 6.2645 mL | |
| 10 mM | 0.3132 mL | 1.5661 mL | 3.1322 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.
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