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ZD 7114 hydrochloride (also known as ZD7114) is a novel, potent and selective beta-adrenoceptor agonist of brown fat and thermogenesis. It has the promise in the treatment of obesity. ICI D7114 stimulates whole body oxygen consumption in conscious rats, cats and dogs and brown adipose tissue (BAT) activity in conscious rats. Treatment of rats with ICI D7114 stimulated oxygen consumption (ED50, 0.04 mg kg-1, p.o.) and BAT mitochondrial guanosine diphosphate (GDP)-binding (ED50, 0.15 mg kg-1, p.o.) with no chronotropic effects on the heart at these doses.
| Targets |
β3-adrenergic receptors
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|---|---|
| ln Vitro |
Increasing energy expenditure by treatment with thermogenic drugs is not new, but available drugs have suffered from the problem of lack of selectivity. In the last decade two key findings have allowed the development of selective thermogenic drugs that have promise in the treatment of obesity. 1) The recognition that brown adipose tissue (BAT) plays a role in compensatory increases in energy expenditure has allowed an approach directed at a target organ. 2) The demonstration showing that increases in the activity of BAT may be modulated by an atypical (beta 3) adrenoceptor has led to the development of a new peripherally acting beta-adrenoceptor agonist ICI D7114, which stimulates thermogenesis at doses that have little effect on beta 1 or beta 2 adrenoceptors. Treatment with the compound activates BAT and thermogenesis even in species and situations where the intrinsic capacity is low. 3) The compound has beneficial effects in animal models of obesity and disturbed glucose and lipid homeostasis. [1]
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| ln Vivo |
ICI D7114 is a potent and selective stimulant of whole body oxygen consumption with little effect on heart rate in the rat. In addition, administration of ICI D7114 did not produce #2-adrenoceptor-mediated effects such as tremor or hypokalaemia. The results suggest that ICI D7114 may be useful in the treatment of obesity and related diseases such as diabetes.[2]
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| Animal Protocol |
rats treated with ICI D7114 or clenbuterol were dosed by gavage with the compounds dissolved in aqueous 0.025% polysorbate. [2]
In the first series, four dogs received gelatin capsules containing 0.1, 1.0 or 10.Omgkg-' of ICI D7114 or a placebo capsule containing lactose. Each dog received each treatment with a washout period of at least one week between treatments. In the second series the effects of 0.01, 0.03 and 0.1 mgkg-t ICI D7114 were compared with placebo. The effects of treatment with placebo capsules or capsules containing 0.1 or 10.0mgkg-' of ICI D7114 were also assessed in five cats in the same way as described for dogs.[2] Dogs with indwelling venous and arterial catheters were dosed with capsules containing ICI D7114 or a placebo preparation of lactose. Blood samples were taken via the catheters at intervals after dosing for the determination of blood potassium with a Nova Stat Profile blood gas analyser.[2] |
| References |
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| Additional Infomation |
1. ICI D7114 is a novel, beta-adrenoceptor agonist which stimulates whole body oxygen consumption in conscious rats, cats and dogs and brown adipose tissue (BAT) activity in conscious rats. Treatment of rats with ICI D7114 stimulated oxygen consumption (ED50, 0.04 mg kg-1, p.o.) and BAT mitochondrial guanosine diphosphate (GDP)-binding (ED50, 0.15 mg kg-1, p.o.) with no chronotropic effects on the heart at these doses. 2. Reference beta-adrenoceptor agonists, isoprenaline and clenbuterol, also stimulated oxygen consumption and BAT activity but were less selective because they also produced effects on heart rate at these doses. 3. Treatment of conscious rats with ICI D7114 did not attenuate the chronotropic effects on the heart of a subsequent isoprenaline challenge. 4. Administration of ICI D7114 or of its acid metabolite had no effect in a cat soleus muscle model of tremor or on blood potassium levels in the conscious dog, indicating lack of effects at beta 2-adrenoceptors. 5. The results indicate that ICI D7114 may have activity at atypical beta-adrenoceptors in brown adipose tissue leading to increased whole body oxygen consumption. [2]
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| Molecular Formula |
C22H30N2O6.HCL
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|---|---|
| Molecular Weight |
454.94434
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| Exact Mass |
454.187
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| Elemental Analysis |
C, 58.08; H, 6.87; Cl, 7.79; N, 6.16; O, 21.10
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| CAS # |
129689-28-7
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| Related CAS # |
129689-30-1;129689-28-7 (HCl);
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| PubChem CID |
9890216
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
3.269
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
15
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| Heavy Atom Count |
31
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| Complexity |
439
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| Defined Atom Stereocenter Count |
1
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| SMILES |
COCCNC(=O)COC1=CC=C(C=C1)OCCNCC(COC2=CC=CC=C2)O.Cl
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| InChi Key |
KCAMZVQSGDBGGF-FERBBOLQSA-N
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| InChi Code |
InChI=1S/C22H30N2O6.ClH/c1-27-13-12-24-22(26)17-30-21-9-7-20(8-10-21)28-14-11-23-15-18(25)16-29-19-5-3-2-4-6-19;/h2-10,18,23,25H,11-17H2,1H3,(H,24,26);1H/t18-;/m0./s1
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| Chemical Name |
2-[4-[2-[[(2S)-2-hydroxy-3-phenoxypropyl]amino]ethoxy]phenoxy]-N-(2-methoxyethyl)acetamide;hydrochloride
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| Synonyms |
ICI-D7114; ICI-D 7114; ICI-D-7114; ZD7114; ZD 7114 hydrochloride; 129689-28-7; D-7114 hydrochloride; ZD-7114 hydrochloride; ZD-7114 (hydrochloride); (S)-4-[2-HYDROXY-3-PHENOXYPROPYLAMINOETHOXY]-N-(2-METHOXYETHYL)PHENOXYACETAMIDE HYDROCHLORIDE; Z63T1D9750; (S)-2-(4-(2-((2-Hydroxy-3-phenoxypropyl)amino)ethoxy)phenoxy)-N-(2-methoxyethyl)acetamide hydrochloride; ZD 7114; ZD7114 HCl; ZD-7114; ZD 7114 hydrochloride
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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) |
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
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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 | 2.1981 mL | 10.9905 mL | 21.9809 mL | |
| 5 mM | 0.4396 mL | 2.1981 mL | 4.3962 mL | |
| 10 mM | 0.2198 mL | 1.0990 mL | 2.1981 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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