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Nylidrin hydrochloride

Alias: Arlidin Hydrochloride; Arlidin; Nylidrin hydrochloride
Cat No.:V21583 Purity: ≥98%
Nylidrin HCl is an inhibitor (blocker/antagonist) of IgE-mediated histamine release from peritoneal mast cells in passively sensitized rats and has anti-allergy effects.
Nylidrin hydrochloride
Nylidrin hydrochloride Chemical Structure CAS No.: 849-55-8
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
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Product Description
Nylidrin HCl is an inhibitor (blocker/antagonist) of IgE-mediated histamine release from peritoneal mast cells in passively sensitized rats and has anti-allergy effects.
Nylidrin hydrochloride (CAS#: 849-55-8, molecular formula C19H26ClNO2, molecular weight 335.87) is a beta-adrenergic agonist. It causes peripheral vasodilation, has a positive inotropic effect, and increases gastric juice volume. It has been used in the treatment of peripheral vascular disorders and premature labor. Nylidrin hydrochloride is also an effective inhibitor of IgE-mediated histamine release.
Biological Activity I Assay Protocols (From Reference)
Targets
Nylidrin hydrochloride is an agonist of β-adrenergic receptors. It binds to β-adrenergic receptors with a Kg of 0.37 μM. It also acts as an antagonist of NR1A/2B subunit-containing NMDA receptors. Additionally, it inhibits IgE-mediated histamine release from mast cells and basophils.
ln Vitro
In vitro, Nylidrin hydrochloride effectively inhibits IgE-mediated release of histamine from passively sensitized rat peritoneal mast cells and human basophils. It also inhibits IgG1-mediated histamine release from passively sensitized guinea pig lung slices. These activities highlight its antiallergic properties.
ln Vivo
Nylidrin hydrochloride has been used as a hypotensive drug in the treatment of arterial hypertension in pregnancy. It has been applied to hypertensive women in advanced pregnancy as a betamimetic for tocolysis. Its vasodilatory effects contribute to its in vivo pharmacological actions.
Enzyme Assay
In vitro enzyme/receptor binding assays for Nylidrin hydrochloride typically involve radioligand binding studies to determine its affinity for β-adrenergic receptors. The Kg value of 0.37 μM is derived from such binding experiments. Functional assays measuring receptor-mediated signaling pathways can also be used.
Cell Assay
In vitro cellular assays for Nylidrin hydrochloride involve studying its effects on histamine release from mast cells and basophils. Cells are passively sensitized with IgE, and the inhibition of histamine release upon compound treatment is measured. These assays quantify the compound's antiallergic activity.
Animal Protocol
In vivo animal experiments for Nylidrin hydrochloride have been performed in rat models to study its effects on histamine release. It has also been used in clinical studies involving hypertensive pregnant women. Its tocolytic and hypotensive effects have been evaluated in these settings.
ADME/Pharmacokinetics
Nylidrin hydrochloride is soluble in DMSO (≥41 mg/mL) and water (~5 mg/mL). It is administered orally or via other routes depending on the indication. Its pharmacokinetic properties, such as absorption and metabolism, are consistent with its use as a therapeutic agent for peripheral vascular disorders and other conditions.
Toxicity/Toxicokinetics
Nylidrin hydrochloride has been shown to be an effective inhibitor of histamine release. It has been used clinically, suggesting an acceptable safety profile for its approved indications. Detailed toxicological data is not provided in the search results, but its use as a therapeutic agent implies established safety parameters.
Additional Infomation
Nylidrin hydrochloride is an alkylbenzene compound belonging to the β-adrenergic agonist class. Nylidrin causes peripheral vasodilation, positive inotropic effects, and increases gastric juice secretion. It is used to treat peripheral vascular disease and preterm birth.
Nylidrin hydrochloride is a beta-adrenergic agonist with peripheral vasodilatory and antiallergic properties. It has been used clinically for peripheral vascular disorders and premature labor. Its mechanism involves β-adrenergic receptor agonism and inhibition of histamine release.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C19H26CLNO2
Molecular Weight
335.87
Exact Mass
335.165
CAS #
849-55-8
PubChem CID
5702098
Appearance
White to off-white solid powder
Melting Point
111ºC
LogP
4.617
Hydrogen Bond Donor Count
4
Hydrogen Bond Acceptor Count
3
Rotatable Bond Count
7
Heavy Atom Count
23
Complexity
296
Defined Atom Stereocenter Count
0
SMILES
Cl.OC1C=CC(C(C(C)NC(CCC2C=CC=CC=2)C)O)=CC=1
InChi Key
CLJHABUMMDMAFA-UHFFFAOYSA-N
InChi Code
InChI=1S/C19H25NO2.ClH/c1-14(8-9-16-6-4-3-5-7-16)20-15(2)19(22)17-10-12-18(21)13-11-17;/h3-7,10-15,19-22H,8-9H2,1-2H3;1H
Chemical Name
4-[1-hydroxy-2-(4-phenylbutan-2-ylamino)propyl]phenol;hydrochloride
Synonyms
Arlidin Hydrochloride; Arlidin; Nylidrin hydrochloride
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, avoid exposure to moisture.
Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ≥ 41 mg/mL (~122.07 mM)
H2O : ~5 mg/mL (~14.89 mM)
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
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*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 : PEG300Tween 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).
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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)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL 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).
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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders


Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.9773 mL 14.8867 mL 29.7734 mL
5 mM 0.5955 mL 2.9773 mL 5.9547 mL
10 mM 0.2977 mL 1.4887 mL 2.9773 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.

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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