Colestilan (MCI-196) is a non-absorbent, non-calcium-based phosphate adhesive and a non-metallic anion exchange resin. Colestilan is orally bioactive and may be utilized in study/research of hypercholesterolemia.

Physicochemical Properties

Molecular Formula	(C4H6N2)N.(C3H5CLO)N
Molecular Weight	174.62800
Exact Mass	174.056
CAS #	95522-45-5
PubChem CID	65840
Appearance	Off-white to light brown solid powder
LogP	1.342
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	2
Rotatable Bond Count	1
Heavy Atom Count	11
Complexity	82.7
Defined Atom Stereocenter Count	0
SMILES	CC1=NC=CN1.ClCC1OC1
InChi Key	DEMLYXMVPJAVFU-UHFFFAOYSA-N
InChi Code	InChI=1S/C4H6N2.C3H5ClO/c1-4-5-2-3-6-4;4-1-3-2-5-3/h2-3H,1H3,(H,5,6);3H,1-2H2
Chemical Name	2-(chloromethyl)oxirane;2-methyl-1H-imidazole
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)

Biological Activity

ln Vitro	Bile acids from the digestive system are absorbed by colonestilan (MCI-196), which lowers cholesterol levels [2]. In vitro, with a phosphate concentration of 2-4 mM and pH 7.2, 1 g of colonestilan binds 2.52 mmol phosphate [2].
ln Vivo	Rats treated with colonestilan (MCI-196) (0.125 g or 0.5 g per 15 g of feed; oral; 14 days) have lower excretions of phosphorus in their serum and urine [3]. In rats given adenine for four weeks, which results in renal failure, colonestilan can alleviate hyperphosphatemia [1].
Animal Protocol	Animal/Disease Models: 6weeks old Wistar male rats [3] Doses: 0.125 or 0.5 grams per 15 grams of feed Route of Administration: Oral administration in feed, 14 days Experimental Results: Dose-dependent reduction of blood phosphorus and urinary phosphorus excretion.
References	[1]. Locatelli F, et al. Effect of MCI-196 on serum phosphate and cholesterol levels in haemodialysis patients with hyperphosphataemia: a double-blind, randomized, placebo-controlled study. Nephrol Dial Transplant. 2010 Feb;25(2):574-81. [2]. Kurihara S, et al. Effect of MCI-196 (colestilan) as a phosphate binder on hyperphosphataemia in aemodialysis patients: a double-blind, placebo-controlled, short-term trial. Nephrol Dial Transplant. 2005 Feb;20(2):424-30. [3]. MATSUKA MASAYUKI, et al. Use of anion exchange resins for the manufacture of a medicament for the treatment of hyperphosphatemia. Patent EP0793960.
Additional Infomation	See also: Colestilan Chloride (annotation moved to). Drug Indication Treatment of hyperphosphataemia in adult patients with chronic kidney disease stage 5 receiving haemodialysis or peritoneal dialysis. Treatment of hyperphosphataemia

Solubility Data

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 (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 : 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). 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 : PEG300：Tween 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). 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	5.7264 mL	28.6320 mL	57.2639 mL
	5 mM	1.1453 mL	5.7264 mL	11.4528 mL
	10 mM	0.5726 mL	2.8632 mL	5.7264 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.